Search Result
Results for "
Nonsmall cell lung cancer (NSCLC)
" in MedChemExpress (MCE) Product Catalog:
7
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-110171
-
iMDK
5 Publications Verification
|
PI3K
|
Cancer
|
|
iMDK is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice .
|
-
-
- HY-112870
-
|
Alflutinib; Furmonertinib; AST2818
|
EGFR
|
Cancer
|
|
Firmonertinib (Alflutinib; Furmonertinib) is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
|
-
-
- HY-P99269
-
|
BIBH 1; Anti-Human FAP Recombinant Antibody
|
FAP
|
Cancer
|
|
Sibrotuzumab (BIBH 1) is a humanized IgG1 monoclonal antibody targets fibroblast activation protein (FAP). Sibrotuzumab can be used for the research of colorectal cancer and non-small cell lung cancer (NSCLC) .
|
-
-
- HY-162307
-
|
|
PROTACs
Keap1-Nrf2
|
Cancer
|
|
Nrf2 degrader 1 (compound 1) is a PROTAC Nrf2 degrader with a DC50 of 0.1-1 μM in huH1 cells. Nrf2 degrader 1 inhibits cancer cells growth for A549 and LK-2 cells with IC50 values of 100 nM and 40 nM, respectively. Nrf2 degrader 1 can be used for the study of liver cancer, non-small cell lung cancer (NSCLC) and squamous cell carcinoma of lung cancer .
|
-
-
- HY-175749
-
|
|
Molecular Glues
Wee1
|
Inflammation/Immunology
Cancer
|
|
BMS-986463, a CRBN E3 ligase modulator (CELMoD), is a WEE1 kinase molecular glue degrader. BMS-986463 significantly inhibits tumor regression and reduces the level of phospho-CDK2. BMS-986463 can be used for advanced malignant solid tumors like non-small cell lung cancer (NSCLC) research .
|
-
-
- HY-147340
-
|
Tirumotecan
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
TL033 is a drug-Linker conjugates for ADC. TL033 contains a linker and bioactive small molecule toxins. TL033 can conjugate with Sacituzumab antibody (anti Trop-2) for synthesizing BT001021. BT001021 has anti-cancer activities against various cancers, such as breast cancer, non-small cell lung cancer (NSCLC), gastric cancer .
|
-
-
- HY-P9986
-
|
MTIG-7192A; RG-6058
|
CD28
|
Cancer
|
|
Tiragolumab is an immune checkpoint inhibitor binding to the T-cell immunoglobulin and ITIM domain (TIGIT). Tiragolumab in combination with Atezolizumab (HY-P9904) and Bevacizumab (HY-P9906) has benefit in unresectable hepatocellular carcinoma. Tiragolumab can be used to study non-small cell lung cancer (NSCLC) and melanoma .
|
-
-
- HY-P10944
-
|
NNS309
|
FAP
|
Inflammation/Immunology
Cancer
|
|
Unlabeled FXX489 (NNS309) is a fibroblast activation protein (FAP)-targeting ligand. Unlabeled FXX489 can be labeled with 68Ga and 177Lu and shows anticancer effects. Unlabeled FXX489 can be used for the study of pancreatic ductal adenocarcinoma (PDAC), non-small cell lung cancer (NSCLC), breast cancer (BC), and colorectal cancer (CRC) .
|
-
-
- HY-112870A
-
|
Alflutinib mesylate; Furmonertinib mesylate; AST2818 mesylate
|
EGFR
|
Inflammation/Immunology
Cancer
|
|
Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and blood-brain barrier penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
|
-
-
- HY-147340A
-
|
Tirumotecan TFA
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
TL033 TFA is a drug-Linker conjugates for ADC. TL033 TFA contains a linker and bioactive small molecule toxins. TL033 TFA can conjugate with Sacituzumab antibody (anti Trop-2) for synthesizing BT001021. BT001021 has anti-cancer activities against various cancers, such as breast cancer, non-small cell lung cancer (NSCLC), gastric cancer .
|
-
-
- HY-144680
-
|
ZL-2313
|
EGFR
|
Cancer
|
|
BLU-945 is a potent, highly selective, reversible and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKIs). BLU-945 can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation and C797S mutation. BLU-945 can be used for the research of lung cancer including non-small cell lung cancer (NSCLC) .
|
-
-
- HY-176857
-
|
|
PROTACs
STAT
|
Inflammation/Immunology
Cancer
|
|
PROTAC STAT6 degrader-1 (Compound I-2) is a potent STAT6 PROTAC degrader with a DC50 <1 nM. PROTAC STAT6 degrader-1 inhibits STAT6 activity with an IC50 of <0.1 pM. PROTAC STAT6 degrader-1 can be used for inflammatory and cancers research, such as non-small cell lung cancer (NSCLC) .
|
-
-
- HY-P99379
-
|
CAN04; Anti-IL-1RAP/IL-1R3 Reference Antibody (nidanilimab)
|
Interleukin Related
|
Cancer
|
|
Nidanilimab (CAN04) is a fully humanized monoclonal anti-IL1RAP antibody with a Kd value of 1.10 pM. Nidanilimab blocks IL1α and IL1β signaling and stimulates the immune system to destroy tumour cells. Nidanilimab can be used in research of non-small lung cancer (NSCLC) and pancreatic ductal adenocarcinoma (PDAC) .
|
-
-
- HY-114358
-
|
ONO-7475
|
TAM Receptor
Trk Receptor
|
Cancer
|
|
Tamnorzatinib (ONO-7475) is a potent, selective, and orally active Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. Tamnorzatinib sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. Tamnorzatinib combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC).
|
-
-
- HY-107553
-
|
|
HSP
Apoptosis
|
Cancer
|
|
Chetomin, an active component of Chaetomium globosum, is a heat shock protein 90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancer cancer stem cells (NSCLC CSC)-targeting molecule .
|
-
-
- HY-13299
-
MK-8033
3 Publications Verification
|
c-Met/HGFR
|
Cancer
|
|
MK-8033 is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
|
-
-
- HY-P99202
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
Vibostolimab is an anti-TIGIT (T cell immunoglobulin and ITIM domain) monoclonal antibody. Vibostolimab shows antitumor activity, and can be used in non-small cell lung cancer (NSCLC) and melanoma research .
|
-
-
- HY-19642A
-
|
MGCD265 hydrochloride
|
TAM Receptor
c-Met/HGFR
|
Cancer
|
|
Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) .
|
-
-
- HY-P5005
-
|
|
CMV
PD-1/PD-L1
|
Infection
Inflammation/Immunology
Cancer
|
|
VIPhyb is a vasoactive intestinal polypeptide (VIP) receptor antagonist. VIPhyb can inhibit VIP signaling, increase T-cell immunity and downregulate PD1. VIPhyb can inhibit cancer cell proliferation. VIPhyb can reduce inflammatory cytokine expression. VIPhyb can enhance viral clearance. VIPhyb can be used for the researches of cancer, infection and inflammation and immunology, such as non-small cell lung cancer (NSCLC), cytomegalovirus infection and colitis .
|
-
-
- HY-N0429
-
|
|
Apoptosis
MDM-2/p53
Bcl-2 Family
CDK
|
Cancer
|
|
Diosbulbin B, a diterpene lactone, is an anticancer agent. Diosbulbin B is an orally active component of Dioscorea. bulbifera L. Diosbulbin B can inhibit cell proliferation, induce G0/G1 phase arrest and apoptosis. Diosbulbin B can induce autophagy and mitochondrial dysfunction. Diosbulbin B can induce liver injury. Diosbulbin B can be used for the research of cancer, such as non-small cell lung cancer (NSCLC) .
|
-
-
- HY-153863
-
|
|
PROTACs
MEK
Raf
|
Cancer
|
|
MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader. MS934 also degrades CRAF. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma (Pink: Target protein ligand (HY-168288); Black: linker (HY-168289); Blue: E3 ligase ligand (HY-112078)) .
|
-
-
- HY-118263
-
|
PF-00299804 hydrate; PF-299804 hydrate
|
EGFR
|
Cancer
|
|
Dacomitinib (PF-00299804) hydrate is an orally active, irreversible pan-ErbB inhibitor. Dacomitinib hydrate can be used in the research of cancers such as metastatic non-small cell lung cancer (NSCLC) .
|
-
-
- HY-P99223
-
|
MEDI-575
|
PDGFR
|
Cancer
|
|
Tovetumab (MEDI-575) is an anti-PDGFRα monoclonal antibody that selectively blocks the PDGFRα signal transduction. Tovetumab can be used in the research of glioblastoma and non-small cell lung cancer (NSCLC) .
|
-
-
- HY-114842
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
TDRL-551 is a potent replication protein A (RPA) inhibitor (IC50 = 18 µM). TDRL-551 inhibits RPA-DNA interaction and increases the anti-cancer efficacy of Platinum (Pt)-based chemotherapy. TDRL-551 can be used for the research of cancer, such as non-small cell lung cancer (NSCLC) .
|
-
-
- HY-P99827
-
|
TSR-022; GSK4069889
|
Tim3
|
Cancer
|
|
Cobolimab (TSR-022) is an anti-TIM-3 monoclonal antibody. Cobolimab mediates the internalization of TIM3 with an IC50 value of 0.4464 nM. Cobolimab has potential application in solid tumors and non-small cell lung cancer (NSCLC) .
|
-
-
- HY-P990049
-
|
JMT-101; MRG003 Antibody
|
EGFR
|
Cancer
|
|
Becotatug (JMT-101) is a humanized IgG1 antibody targeting EGFR. Becotatug can also be conjugated to Afatinib (HY-10261) and Osimertinib (HY-15772) as a synthetic ADC. Becotatug can be used for the study of EGFR-mutated advanced non-small cell lung cancer (NSCLC) .
|
-
-
- HY-P99785
-
|
HLX20; HLX43 antibody
|
PD-1/PD-L1
ADC Antibody
|
Cancer
|
|
Opucolimab (HLX20) is an engineered anti-PD-L1 humanised IgG1 antibody. Opucolimab, when conjugated with camptothecin toxoid, yields the PD-L1-targeting ADC, HLX43 (HY-177439). HLX43 can be used for non-small cell lung cancer (NSCLC), head and neck squamous cell carcinoma (HNSCC), esophageal squamous cell carcinoma (ESCC), melanoma (MEL), ovarian cancer (Ovc) research .
|
-
-
- HY-117366
-
|
|
PKC
|
Cancer
|
|
PS432 is a PKC inhibitor with IC50s of 16.9 μM (PKCι) and 18.5 μM (PKCζ), respectively. PS432 effectively inhibits the proliferation of non-small cell lung cancer cells (NSCLCs) and tumor growth in mouse xenograft models .
|
-
-
- HY-147259
-
|
|
c-Met/HGFR
|
Cancer
|
|
Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC) .
|
-
-
- HY-151606
-
|
|
Akt
|
Cancer
|
|
Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomesOsimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer .
|
-
-
- HY-P99705
-
|
RG-7599; DNIB-0600A; NaPi2b-ADC
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
Lifastuzumab vedotin (RG-7599; DNIB0600A) is an antibody-drug conjugate (ADC) that comprises a humanized IgG1 anti-NaPi2b monoclonal antibody (MNIB2126A) and a potent antimitotic agent, monomethyl auristatin E (MMAE), which inhibits cell division by blocking the polymerization of tubulin. Lifastuzumab vedotin has the potential for non-small cell lung cancer (NSCLC) and platinum-resistant ovarian cancer (PROC) research .
|
-
-
- HY-164426
-
HEI3090
1 Publications Verification
|
P2X Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
Cancer
|
|
HEI3090 is a P2X7R activator. HEI3090 stimulates dendritic cells expressing P2X7R to produce IL-18, which subsequently promotes Natural Killer cells and CD4 T cells within tumors to produce IFN-γ, leading to a sustained antitumor response. HEI3090 can be used to enhance the efficacy of αPD-1 therapy in non-small cell lung cancer (NSCLC) .
|
-
-
- HY-148803
-
|
|
c-Met/HGFR
|
Cancer
|
|
Vabametkib is a MET TKI inhibitor. Vabametkib can be used in research on non-small cell lung cancer (NSCLC) .
|
-
-
- HY-176205
-
|
AB801
|
TAM Receptor
|
Cancer
|
|
Ligritinib (AB801) is an orally active AXL receptor tyrosine kinase inhibitor. Ligritinib blocks the downstream signaling pathway by inhibiting the kinase activity of AXL. Ligritinib can be used in cancer research, especially in combination with chemotherapy for non-small cell lung cancer (NSCLC) .
|
-
-
- HY-110171A
-
|
|
PI3K
|
Cancer
|
|
iMDK quarterhydrate is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK quarterhydrate suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice .
|
-
-
- HY-19637
-
|
|
Topoisomerase
|
Cancer
|
|
SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.
|
-
-
- HY-19642
-
|
MGCD265
|
TAM Receptor
c-Met/HGFR
|
Cancer
|
|
Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) .
|
-
-
- HY-P99921
-
|
HuMax-AXL-ADC
|
Antibody-Drug Conjugates (ADCs)
TAM Receptor
|
Cancer
|
|
Enapotamab vedotin is an AXL-targeted antibody-drug conjugate (ADC) with inhibitory potential against high AXL expressing non-small cell lung cancer (NSCLC). Enapotamab vedotin also exhibits resistant to EGFR inhibitor such as Osimertinib (HY-15772) .
|
-
-
- HY-W423595
-
|
|
EGFR
|
Cancer
|
|
BEBT-109 is a potent pan-mutant-selective EGFR inhibitor. BEBT-109 has improved pharmacokinetic properties. BEBT-109 can be used for multiple mutant-EGFR-driven non-small cell lung cancer (NSCLC) research .
|
-
-
- HY-147281
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
BAY 1135626 is used to synthesize BAY 1129980, and use to anti-tumor research. BAY 1129980 is a Auristatin-based anti-C4.4A (LYPD3) antibody–agent conjugate (ADC), is used to non–small cell lung cancer (NSCLC) research .
|
-
-
- HY-138751A
-
|
ASK120067 diTFA
|
EGFR
|
Cancer
|
|
limertinib (ASK120067) diTFA is a potent and orally active inhibitor of EGFR T790M (IC50: 0.3 nM) with selectivity over EGFR WT (IC50: 6.0 nM). limertinib diTFA is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC) .
|
-
-
- HY-124084
-
|
|
Stearoyl-CoA Desaturase (SCD)
|
Cancer
|
|
SW203668 is an irreversible stearoyl CoA desaturase (SCD) inhibitor with an IC50 of 54 nM. SW203668 covalently binds and inhibits SCD, depletes unsaturated fatty acids, and triggers cell death in sensitive cells. SW203668 requires demethylation by CYP4F11 to form its active SCD-inhibiting form; differential CYP4F11 expression drives selective cytotoxicity. SW203668 exerts cytotoxicity toward CYP4F11-expressing non-small cell lung cancer (NSCLC) cells and spares CYP4F11-lacking NSCLC cells. SW203668 inhibits tumor growth in immunodeficient mice bearing CYP4F11-expressing NSCLC xenografts and spares mouse skin sebocytes. SW203668 can be used for the research of non-small cell lung cancer .
|
-
-
- HY-18030A
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
CEP-28122 mesylate salt, a diaminopyrimidine derivative, is a potent, selective, and orally active ALK inhibitor with an IC50 value of 1.9 nM. CEP-28122 mesylate salt has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate salt has good pharmacodynamic and pharmacokinetic activity. CEP-28122 mesylate salt can be used for the study of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells .
|
-
-
- HY-18030
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
CEP-28122, a diaminopyrimidine derivative, is a potent, selective, and orally active ALK inhibitor with an IC50 value of 1.9 nM. CEP-28122 has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 has good pharmacodynamic and pharmacokinetic activity. CEP-28122 can be used for the study of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells .
|
-
-
- HY-175837
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-172 is a EGFR inhibitor. EGFR-IN-172 effectively inhibits the proliferation of non-small cell lung cancer (NSCLC) cells carrying the L858R, T790M and C797S drug-resistant mutations. EGFR-IN-172 inhibits EGFR phosphorylation, induces cell cycle arrest and apoptosis. EGFR-IN-172 can be used for the study of NSCLC .
|
-
-
- HY-W001983
-
|
|
Dihydropyrimidine Dehydrogenase (DPD)
|
Cancer
|
|
5-Iodouracil (Compound 4b) is an irreversible dihydropyrimidine dehydrogenase (DPD) inhibitor (IC50=0.22 μM). 5-Iodouracil is promising for research of DPD-overexpressing solid tumors like non-small cell lung cancer (NSCLC) .
|
-
-
- HY-123766
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-99 (compound 1a) is a potent EGFR and HER2 Exon 20 insertion mutant inhibitor. EGFR-IN-99 has excellent antiproliferative activity against DFCI127 cells, with an EC50 of 11.5 nM. EGFR-IN-99 can be used for the research of non-small cell lung cancer (NSCLC) .
|
-
-
- HY-179143
-
|
|
EGFR
Akt
Apoptosis
|
Cancer
|
|
EGFR-IN-185 is a EGFR inhibitor. EGFR-IN-185 exhibits potent activity against non-small cell lung cancer (NSCLC) cells harboring EGFR mutations. EGFR-IN-185 inhibits colony formation and migration, induces G0/G1 arrest, and promots apoptosis, which are associated with the suppression of EGFR and AKT phosphorylation. EGFR-IN-185 can be used for the research of NSCLC .
|
-
-
- HY-151377
-
|
|
RET
EGFR
Aurora Kinase
c-Fms
MAP4K
|
Cancer
|
|
RET-IN-19 (compound 59) is a potent RET inhibitor, with IC50 values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research .
|
-
-
- HY-143466
-
|
|
FAK
ULK
AMPK
Apoptosis
Autophagy
|
Cancer
|
|
ULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC50 of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy, and can be used to study NSCLC (Non-small cell lung cancer) .
|
-
- HY-173403
-
|
|
TrxR
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
TrxR-IN-8 (Compound 6f) is a selective TrxR inhibitor (IC50: 10.2 μM). TrxR-IN-8 induces apoptosis through oxidative stress by stimulating the production of reactive oxygen species (ROS), reducing intracellular thiols, and lowering the glutathione/glutathione ratio. TrxR-IN-8 exhibits significant cytotoxicity against non-small cell lung cancer (NSCLC) cells .
|
-
- HY-106219
-
|
|
Microtubule/Tubulin
P-glycoprotein
|
Cancer
|
|
BMS 275183 is a potent, orally active analogue of Paclitaxel (HY-B0015). BMS 275183 can stabilize microtubules and exhibits antitumor activity in in vivo tumor models. BMS 275183 is active in vitro against Paclitaxel-resistant tumors including those harboring tubulin mutations or overexpressing P-glycoprotein. BMS 275183 can be used for cancer research, such as non-small cell lung cancer (NSCLC) and prostate carcinoma .
|
-
- HY-164513
-
|
|
Ras
Phosphodiesterase (PDE)
|
Cancer
|
|
NHTD is a KRAS-PDEδ inhibitor. NHTD targets the prenyl-binding pocket of PDEδ, altering the cellular localization of KRAS, thereby inhibiting the proliferation of KRAS-mutant cancer cells and inducing apoptosis. NHTD can be used for research on KRAS-driven non-small cell lung cancer (NSCLC) .
|
-
- HY-147802
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-59 (Compound 8c) is a EGFR inhibitor (IC50=190 nM) and apoptosis inducer. EGFR-IN-59 exhibits cytotoxicity against non-small lung cancer cell lines (A549) and normal lung fibroblasts (WI38) with IC50s of 8.62 and 52.6 µM, respectively. EGFR-IN-59 can be used for the research of various cancers such as non-small cell lung cancer (NSCLC), head and neck cancer, breast cancer and colorectal cancer .
|
-
- HY-P991635
-
|
|
TNF Receptor
|
Cancer
|
|
PF-07329640 is a humanized monoclonal antibody inhibitor targeting TNFRSF3. PF-07329640 can be used for advanced/metastatic solid tumors like non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) research .
|
-
- HY-119182
-
|
NSC 300288
|
DNA/RNA Synthesis
|
Cancer
|
|
Mitonafide (NSC 300288) is a cytostatic agent. Mitonafide binds to double-stranded DNA through intercalation, and inhibits DNA and RNA synthesis. Mitonafide is an antitumor agent that can be used in the research of cancers, such as non-small cell lung cancer (NSCLC), leukemia .
|
-
- HY-168874
-
|
|
TrxR
Apoptosis
Ferroptosis
|
Cancer
|
|
TrxR1-IN-2 (Compound 6a) is a TrxR1 inhibitor that covalently binds to the Cys475 and Sec498 sites of TrxR1, thereby inhibiting TrxR1 activity and leading to redox homeostasis disruption, which triggers apoptosis and ferroptosis .
|
-
- HY-P991612
-
|
Sym024
|
CD73
|
Inflammation/Immunology
Cancer
|
|
S095024 is a humanized IgG1 monoclonal antibody inhibitor targeting CD73. S095024 can be used to study acute respiratory distress syndrome (ARDS), non-small cell lung cancer (NSCLC) and advanced solid tumor malignancies .
|
-
- HY-P991244
-
|
|
EGFR
|
Cancer
|
|
REGN-1400 is a humanized monoclonal antibody inhibitor targeting ErbB3. REGN-1400 reduces tumor cell proliferation by inhibiting ErbB3 and blocking related signaling pathways. REGN-1400 is promising for research of solid tumors such as non-small cell lung cancer (NSCLC), colorectal cancer (CRC), and squamous cell carcinoma of the head and neck (SCCHN) .
|
-
- HY-13299A
-
|
|
c-Met/HGFR
|
Cancer
|
|
MK-8033 hydrochloride is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 hydrochloride can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
|
-
- HY-179536
-
|
|
Ras
|
Cancer
|
|
KRAS-IN-49 (compound 7b) is a selective and covalent KRAS G13C inhibitor. KRAS-IN-49 covalently binds to Cys13 of KRAS G13C. KRAS-IN-49 can be used for non-small cell lung cancer (NSCLC) research .
|
-
- HY-P991058
-
|
BMS-986315
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
Zimistobart (BMS-986315) is a fully human IgG1 antibody that targets NKG2A. Zimistobart can be used for the study of non-small cell lung cancer (NSCLC). The isotype control for Zimistobart can refer to Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-124084A
-
|
|
Stearoyl-CoA Desaturase (SCD)
|
Cancer
|
|
SW203668 TFA is an irreversible stearoyl CoA desaturase (SCD) inhibitor with an IC50 of 54 nM. SW203668 TFA covalently binds and inhibits SCD, depletes unsaturated fatty acids, and triggers cell death in sensitive cells. SW203668 TFA requires demethylation by CYP4F11 to form its active SCD-inhibiting form; differential CYP4F11 expression drives selective cytotoxicity. SW203668 TFA exerts cytotoxicity toward CYP4F11-expressing non-small cell lung cancer (NSCLC) cells and spares CYP4F11-lacking NSCLC cells. SW203668 TFA inhibits tumor growth in immunodeficient mice bearing CYP4F11-expressing NSCLC xenografts and spares mouse skin sebocytes. SW203668 TFA can be used for the research of non-small cell lung cancer .
|
-
- HY-158058
-
|
|
Toll-like Receptor (TLR)
Pyroptosis
|
Inflammation/Immunology
Cancer
|
|
WYJ-2 is a selective agonist for toll-like receptor 2/1 (TLR2/1) with EC50 of 18.57 nM in human TLR2 and TLR1 transient-cotransfected HEK 293T cells. WYJ-2 induces pyroptosis and exhibits anticancer activity against non-small cell lung cancer (NSCLC) .
|
-
- HY-P991620
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
JS006 is a humanized IgG4κ monoclonal antibody inhibitor targeting TIGIT/CD155. JS006 can be used to study advanced and/or metastatic cancers with resistance to PD-1/PD-L1 inhibitor such as non-small cell lung cancer (NSCLC), advanced lymphoma and advanced/metastatic triple negative breast cancer (TNBC) .
|
-
- HY-170438
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-139 (compound PD 18) is an epidermal growth factor receptor (EGFR) inhibitor, with IC50s of 12.88 (wild type), 10.84 (L858R/T790M), 42.68 (L858R/T790M/C797S) nM, respectively. EGFR-IN-139 displays strong anticancer activity against A549 and H1975 cancer cell lines, which are highly expressed EGFR. EGFR-IN-139 has a strong selectivity to cancer cells. EGFR-IN-139 can be used for nonsmall cell lung cancer (NSCLC) research[1].
|
-
- HY-17667
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-95 (Compound 9) is a HDAC inhibitor. HDAC-IN-95 can be used for the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-151571
-
|
|
Ras
|
Cancer
|
|
ZG1077 is a covalent KRAS G12C inhibitor. ZG1077 can be used in the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-N11912
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Soladulcoside A is a steroidal glycoside and antineoplastic agent that can be obtained from the whole plant of Solanum nigrum. Soladulcoside A can inhibit A549 cells and has the potential to study cancers such as non-small cell lung cancer (NSCLC) .
|
-
- HY-106618
-
|
RA 233
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Mopidamol (RA 233), a derivative of Dipyridamole (HY-B0312), is a phosphodiesterase inhibitor. Mopidamol can be used for non-small cell lung cancer (N-SCLC) research .
|
-
- HY-173501
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-157 (compound IIB-5) is a potent EGFR inhibitor with an IC50 of 18.81 nM. EGFR-IN-157 can be used in the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-169269
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2 degrader-18 (Example144) is a PROTAC SMARCA2 degrader. PROTAC SMARCA2 degrader-18 has the potential for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-19315
-
|
|
Ras
|
Cancer
|
|
SML-8-73-1 is a nucleotide-based KRAS G12C inhibitor. SML-8-73-1 can be used for the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-111261
-
|
|
Autophagy
|
Cancer
|
|
UNBS3157 is a naphthalimide derivative that shows potent anticancer effect. UNBS3157 induces autophagy and senescence in cancer cells. UNBS3157 displays significant antitumor effects in vivo. UNBS3157 can be used for leukemia, mammary adenocarcinoma, non-small cell lung cancer (NSCLC) and pancreatic cancer research .
|
-
- HY-N3764
-
|
|
Akt
Dihydrofolate reductase (DHFR)
Endogenous Metabolite
|
Others
|
|
Diosbulbin C is a diterpene lactone component, which can be extracted from traditional Chinese medicine Dioscorea bulbifera L.. Diosbulbin C possesses high anticancer activity in non-small cell lung cancer (NSCLC). Diosbulbin C could induce cell cycle arrest at G0/G1 phase in NSCLC. Diosbulbin C also inhibits the proliferation of NSCLC cells, possibly by downregulating the expression/activation of AKT, DHFR, and TYMS .
|
-
- HY-152143
-
|
Tubulin polymerization-IN-41
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
KY216 (Tubulin polymerization-IN-41) is a potent tubulin polymerization inhibitor with the IC50 of 2.61 μM. KY216 targets the Colchicine-binding site of tubulin. KY216 can be used for the study of non-small cell lung cancer (NSCLC) and breast cancer .
|
-
- HY-N13164
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
Polygalacin D3 is a triterpenoid saponin compound that can be extracted from the roots of the balloon flower. Polygalacin D3 can inhibit the proliferation of non-small cell lung cancer (NSCLC) cell lines by blocking the PI3K/Akt pathway, and it induces cell cycle arrest and cell apoptosis .
|
-
- HY-161030
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-92 (compound 15) is an allosteric T790M/L858R double mutant EGFR inhibitor. EGFR-IN-92 shows antiproliferative activity against H1975 non-small lung cancer (NSCLC) cancer cells expressing double mutant EGFR .
|
-
- HY-77493
-
|
(rel)-ARQ 197; (rel)-(3R,4R)-ARQ 198
|
c-Met/HGFR
|
Cancer
|
|
(rel)-Tivantinib is a potent and highly selective inhibitor of the receptor tyrosine kinase c-MET. (rel)-Tivantinib has two novel targets, GSK3α and GSK3β, which play an important role in the cellular mechanism of non-small cell lung cancer (NSCLC) .
|
-
- HY-163657
-
|
|
EGFR
|
Cancer
|
|
HER2-IN-20 (compound 32) is a potent and selective HER2 WT and HER2 YVMA inhibitor with IC50 values of 49, 42 nM, respectively. HER2-IN-20 has the potential for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-178386
-
|
|
BCRP
|
Cancer
|
|
ABCG2-IN-5 (Compound 10) is a is a selective ABCG2 inhibitor, with an IC50 of 0.34 µM. ABCG2-IN-5 can be used for the study of ABCG2-overexpressing tumors such as non-small cell lung cancer (NSCLC) .
|
-
- HY-172881
-
|
|
Pyruvate Kinase
|
Cancer
|
|
PKM2-IN-10 (Compound 16) is a PKM2 inhibitor. PKM2-IN-10 inhibits the proliferation of A549 and HCC1833 cell lines with IC50 of 3.36 μM and 9.20 μM, respectively. PKM2-IN-10 exhibits antitumor activity in human non-small cell lung cancer (NSCLC) and mouse lung adenocarcinoma models. PKM2-IN-10 can be used in lung cancer research .
|
-
- HY-119182R
-
|
NSC 300288 (Standard)
|
DNA/RNA Synthesis
Reference Standards
|
Cancer
|
|
Mitonafide (Standard) is the analytical standard of Mitonafide. This product is intended for research and analytical applications. Mitonafide (NSC 300288) is a cytostatic agent. Mitonafide binds to double-stranded DNA through intercalation, and inhibits DNA and RNA synthesis. Mitonafide is an antitumor agent that can be used in the research of cancers, such as non-small cell lung cancer (NSCLC), leukemia .
|
-
- HY-175634
-
|
|
Lipoxygenase
β-catenin
STAT
Apoptosis
|
Cancer
|
|
ALOX5 stabilizer-1 is an arachidonate 5-lipoxygenase (ALOX5) stabilizer with a Kd of 7.26 μM. ALOX5 stabilizer-1 inhibits β-catenin protein levels and then suppresses STAT3 signal pathway. ALOX5 stabilizer-1 induces lung cancer cells apoptosis, inhibited cell migration and proliferation. ALOX5 stabilizer-1 can used for the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-172943
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
PLK1/PRC1-IN-1 (compound B4) is a PLK1/PRC1 protein complex formation inhibitor. PLK1/PRC1-IN-1 can be used in the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-170809
-
|
|
RET
|
Cancer
|
|
RET-IN-29 (Compound 8W) is a selective RET kinase inhibitor. RET-IN-29 exhibits inhibitory potency against the BaF3 cells harboring CCDC6-RET V804M mutation with an IC50 value of 0.715 μM. RET-IN-29 is promising for research of non-small cell lung cancer (NSCLC) .
|
-
- HY-170968
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-150 is an EGFR inhibitor that effectively suppresses the phosphorylation of mutant epidermal growth factor receptor (EGFR) and its downstream AKT signaling pathway, thereby exerting antitumor effects and inducing HMOX1 expression to trigger ferroptosis. EGFR-IN-150 exhibits an IC50 of 0.386 μM against the non-small cell lung cancer (NSCLC) cell line H1975, and significantly inhibits colony formation and migration of both H1975 and A549 cells while inducing apoptosis. In addition, EGFR-IN-150 markedly suppresses tumor growth in the H1975 cell-derived xenograft (CDX) mouse model. EGFR-IN-150 holds promise for research related to non-small cell lung cancer .
|
-
- HY-18030B
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Others
|
|
CEP-28122 mesylate hydrochloride, a diaminopyrimidine derivative, is a potent, selective, and orally active ALK inhibitor with an IC50 value of 1.9 nM. CEP-28122 mesylate hydrochloride has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate hydrochloride has good pharmacodynamic and pharmacokinetic activity. CEP-28122 mesylate hydrochloride can be used for the study of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells .
|
-
- HY-182052
-
|
|
Glutathione Peroxidase
Reactive Oxygen Species (ROS)
NO Synthase
Ferroptosis
Apoptosis
|
Cancer
|
|
anti-NSCLC agent-2 exhibits nanomolar anti-proliferative activity and acts on wild-type and drug-resistant non-small cell lung cancer (NSCLC) cells. anti-NSCLC agent-2 downregulates ferroptosis-related factors SLC7A11 and GPX4, disrupts cellular redox homeostasis, depletes glutathione, accumulates lipid peroxides, and simultaneously elevates mitochondrial nitric oxide and ROS levels to induce ferroptosis in tumor cells. anti-NSCLC agent-2 is applicable to research related to non-small cell lung cancer .
|
-
- HY-114563
-
|
dFdG
|
Drug Derivative
|
Cancer
|
|
LY 223592 (Compound I-a) is a Gemcitabine (HY-17026) derivative. LY 223592 has the biological activity of highly selective inhibition of lung cancer cell proliferation (IC50 = 5.6 nM in A549 cells) and low cytotoxicity to normal cells. LY 223592 can be used for the research of cancer, such as non-small cell lung cancer (NSCLC) .
|
-
- HY-129223A
-
|
|
Drug Derivative
|
Cancer
|
|
28-O-Tigloylgymnemagenin (I) is a natural anticancer agent. 28-O-Tigloylgymnemagenin has good anti-proliferation activity on human acute myeloid leukemia cells and non-small cell lung cancer (NSCLC). 28-O-Tigloylgymnemagenin can be used for the study of leukemia and lung cancer .
|
-
- HY-P991883
-
|
Licartin; Metuximab; Mehuzumab
|
Apoptosis
CDK
Caspase
Bcl-2 Family
|
Cancer
|
|
Metuzumab (Licartin) is a human-mouse chimeric IgG1 monoclonal antibody targeting CD147. Metuzumab induces Apoptosis, reduces levels of Cyclin D1, full-length Caspase-3, and Bcl-2, and increases Bax expression. Metuzumab enhances the sensitivity of non-small cell lung cancer (NSCLC) cells to Gemcitabine (HY-17026). Metuzumab is applicable for research on hepatocellular carcinoma and non-small cell lung cancer [1] [2].
|
-
- HY-179481
-
|
|
Ferroptosis
Keap1-Nrf2
Glutathione Peroxidase
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Ferroptosis inducer-13 is a 5′-prenylated chalcone derivative that effectively induces ferroptosis in human non-small cell lung cancer (NSCLC) cells by altering the activity of the Nrf2/xCT/GPX4 pathway. Ferroptosis inducer-13 exhibits potent anti-proliferative effects in vitro, and inhibits tumour growth in a NSCLC mouse model. Ferroptosis inducer-13 can be used for NSCLC research .
|
-
- HY-119869
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Anaxirone is an anti-tumor agent. The epoxy group in its structure can interfere with the proliferation of tumor cells by alkylating biological macromolecules such as DNA. Anaxirone has dose-limiting toxicity (DLT) and gastrointestinal toxicity. Anaxirone can be used for research on solid tumors such as non-small cell lung cancer (NSCLC) .
|
-
- HY-179534
-
|
|
Ras
|
Cancer
|
|
G13Ci-22 is a MRTX1133 (HY-134813) based KRAS G13C inhibitor. G13Ci-22 can be used for non-small cell lung cancer (NSCLC) research .
|
-
- HY-179699
-
|
|
Caspase
Apoptosis
|
Cancer
|
|
Procaspase-3 activator 1 is a potent procaspase-3 activator. Procaspase-3 activator directly activates procaspase-3 through zinc chelation, thereby inducing apoptosis and inhibiting cancer cell proliferation. Procaspase-3 activator 1 can be used for the research of non-small cell lung cancer (NSCLC) and melanoma .
|
-
- HY-177895
-
|
|
EGFR
|
Cancer
|
|
IAM1363 is a selective, irreversible and brain-penetrant HER2 inhibitor. IAM1363 shows over 1,000-fold selectivity for HER2 compared to EGFR. IAM1363 can be used for the study of advanced HER2 cancers, such as HER2-driven non-small cell lung cancer (NSCLC) .
|
-
- HY-182914
-
|
|
EGFR
Akt
Bcl-2 Family
Apoptosis
|
Cancer
|
|
NGI‑189 is a selective OST‑A inhibitor. NGI‑189 inhibits the STT3A catalytic subunit of the OST complex and reduces N‑glycosylation of target glycoproteins. NGI‑189 blocks oncogenic and bypass signaling, reduces phosphorylation of EGFR, AKT, p70S6K and S6RP, and induces cell cycle arrest and apoptosis. NGI‑189 markedly suppresses tumor growth and induces tumor regression in non‑small cell lung cancer (NSCLC) xenograft models. NGI‑189 can be used for the research of EGFR‑mutant non‑small cell lung cancer .
|
-
- HY-173118
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-152 (compound D4) is a potent EGFR tyrosine kinase inhibitor, exhibiting potent EGFR L858R/T790M/C797S inhibition activity (IC50 = 40 nM). EGFR-IN-152 induces G0/G1 phase cell cycle arrest and apoptosis, thereby inhibiting colony formation and cell proliferation of non-small cell lung cancer (NSCLC) cells. EGFR-IN-152 can be used for NSCLC research .
|
-
- HY-183682
-
|
|
EGFR
p38 MAPK
ERK
Akt
|
Cancer
|
|
AZ14289671 is an orally active, blood-brain barrier-penetrant tyrosine kinase (tyrosine kinase) inhibitor (TKI) that specifically targets non-small cell lung cancer (NSCLC) harboring EGFR exon 20 insertion mutations (EGFR Exon20Ins), while largely sparing wild-type EGFR to reduce off-target toxicities such as rash and diarrhea. AZ14289671 inhibits the downstream MAPK/ERK/AKT pathway, suppressing tumor cell proliferation, survival and migration. AZ14289671 can be used for NSCLC research .
|
-
- HY-111033
-
|
|
MEK
ERK
Apoptosis
p38 MAPK
CDK
PARP
|
Inflammation/Immunology
Cancer
|
|
RO5068760 is a potent, orally active and selective non-ATP-competitive MEK1/2 inhibitor with an IC50 of 0.025 μM for MEK1. RO5068760 significantly inhibits MAPK pathway activity, thereby inducing G1 cell cycle arrest and apoptosis to inhibit cancer cell growth. RO5068760 exhibits significant efficacy in a broad spectrum of tumors with aberrant MAPK pathway activation. RO5068760 can be used for melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer research .
|
-
- HY-109189A
-
|
BPI-7711 hydrochloride
|
EGFR
|
Cancer
|
|
Rezivertinib (BPI-7711) hydrochloride is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib hydrochloride exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib hydrochloride has excellent central nervous system (CNS) penetration and has antitumor activity, such as non-small cell lung cancer (NSCLC) .
|
-
- HY-19815
-
|
CK-101; RX518
|
EGFR
|
Cancer
|
|
Olafertinib (CK-101) is an orally available, third generation and irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). Olafertinib selectively inhibits both EGFR-TKI-sensitizing and resistance mutations with minimal activity on wild-type EGFR. Olafertinib can be used in research for non-small cell lung cancer (NSCLC) with EGFR mutations and other advanced malignancies .
|
-
- HY-50687
-
|
(3S,4S)-ARQ 197; ARQ 198
|
c-Met/HGFR
|
Cancer
|
|
(3S,4S)-Tivantinib is a potent and highly selective inhibitor of the receptor tyrosine kinase c-MET. (3S,4S)-Tivantinib has two novel targets, GSK3α and GSK3β, which play an important role in the cellular mechanism of non-small cell lung cancer (NSCLC) .
|
-
- HY-157526
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-TK-IN-1 (compound 7o) is a potent mutant EGFR inhibitor with IC50 of 8.5 nM an 9.3 nM against EGFR L858R/T790M and EGFR Del19.EGFR-TK-IN-1 showes strong antiproliferative effects against EGFR mutant-driven non-small cell lung cancer (NSCLC) cells and induces cell apoptosis .
|
-
- HY-172429A
-
|
ORIC-114 hemihydrate
|
EGFR
|
Neurological Disease
Cancer
|
|
Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .
|
-
- HY-172429
-
|
ORIC-114
|
EGFR
|
Neurological Disease
Cancer
|
|
Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .
|
-
- HY-121537
-
|
|
COX
Akt
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities .
|
-
- HY-179702
-
|
|
Ras
PERK
Akt
Reactive Oxygen Species (ROS)
Apoptosis
Mitochondrial Metabolism
|
Cancer
|
|
KD36 is a selective KRAS-G12C inhibitor with an IC50 value of 0.92 μM. KD36 can inhibit the phosphorylation of ERK and AKT, induce the accumulation of reactive oxygen species (ROS), reduce mitochondrial membrane potential, thereby leading to apoptosis of KRAS-G12C mutant cells. KD36 can be used in the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-161470
-
|
|
Histone Demethylase
E1/E2/E3 Enzyme
DNA/RNA Synthesis
Caspase
Apoptosis
|
Cancer
|
|
WS-384 is a dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor with oral activity, with IC50 values of 338.79 nM and 14.81 nM, respectively. WS-384 possesses anticancer activity and can cause cell cycle arrest, DNA damage, and induce apoptosis. WS-384 can be used in the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-153356
-
|
|
Molecular Glues
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
MRT-2359 is an orally active and selective GSPT1 molecular glue degrader, with a DC50 of 5 nM. MRT-2359 induces CRBN/GSPT1 ternary complex formation to drive CRBN- and degron-dependent proteasomal GSPT1 degradation, with selectivity for wild-type GSPT1 over the GSPT1G575N mutant. MRT-2359 disrupts protein translation, induces ribosome stalling, downregulates MYC family proteins and their transcriptional output, reduces proliferation, and induces apoptosis in cancer cells. MRT-2359 can be used for the research of non-small cell lung cancer (NSCLC), small cell lung cancer (SCLC), neuroendocrine lung cancer, high grade neuroendocrine cancers, diffuse large B-cell lymphoma, prostate cancer, and MYC-driven solid tumors .
|
-
- HY-125847
-
|
|
Ras
PI3K
Akt
Caspase
Apoptosis
Bcl-2 Family
NF-κB
MMP
|
Cancer
|
|
Salvianolic acid F is a KRAS inhibitor, especially for KRAS G12D. Salvianolic acid F inhibits NF-kB, MMP-9, and NO simultaneously. Salvianolic acid F inhibits cancer cell growth, invasion, and migration and induces apoptosis via the EP300/PI3K/AKT pathway in vitro. Salvianolic acid F inhibits the growth of KRAS-dependent lung cancer cells via the PI3K/AKT signaling pathway in vivo. Salvianolic acid F can be used in the research of various cancers, including KRAS G12D-driven non-small cell lung cancer (NSCLC) and ovarian cancer .
|
-
- HY-P991669
-
|
AML-01
|
Caspase
Apoptosis
|
Cancer
|
|
IGN523 is an anti-CD98 antibody (hCD98, KD = 0.55 nM). IGN523 induces antibody-dependent cell-mediated cytotoxicity (ADCC) activity, lysosomal membrane permeabilization, and inhibition of essential amino acid transport, ultimately leading to caspase-3 and caspase-7-mediated apoptosis of tumor cells. IGN523 inhibits tumor growth in multiple tumor xenograft models. IGN523 is useful in the research of non-small cell lung cancer (NSCLC), acute myeloid leukemia (AML), and other cancers. .
|
-
- HY-119307
-
|
TMI-005
|
MMP
TNF Receptor
|
Cancer
|
|
Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC) . Apratastat is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-162100
-
|
|
ULK
Autophagy
|
Cancer
|
|
MR-2088 is a reversible, ATP-competitive, and selective ULK1/2 inhibitor with pEC50 values of 8.3 and 8.7 respectively. MR-2088 effectively inhibits autophagic flux and demonstrates a synergistic antiproliferative effect with Trametinib (HY-10999) (MEK inhibitor) in vitro. MR-2088 can be used for non-small lung cell cancer (NSCLC) research .
|
-
- HY-19939S
-
VX-984
4 Publications Verification
M9831
|
DNA-PK
|
Cancer
|
|
VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium .
|
-
- HY-153361
-
|
|
PROTACs
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
|
YD23 is a selective SMARCA2 PROTAC degrader with DC50 values of 64 nM and 297 nM in H1792 cells and H1975 cells. YD23 induces degradation of SMARCA2, which is synthetic lethal to SMARCA4. YD23 reduces chromatin accessibility only in SMARCA4 deficient cells, including cell cycle and cell growth regulatory genes. YD23 selectively inhibits growth of SMARCA4 mutant lung cancer cells. YD23 has potent tumor growth inhibitory activity in SMARCA4-mutant xenografts. YD23 can be used for the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-112870AS
-
|
Alflutinib-d3 mesylate; Furmonertinib-d3 mesylate; AST2818-d3 mesylate
|
Isotope-Labeled Compounds
EGFR
|
Inflammation/Immunology
Cancer
|
|
Firmonertinib-d3 (Alflutinib-d3) mesylate is the deuterium labeled Firmonertinib mesylate (HY-112870A). Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and blood-brain barrier penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation.
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-
- HY-114253
-
|
|
EGFR
|
Cancer
|
|
ODS-2004436 is a small molecule radiotracer that uses positron emission tomography (PET) imaging to measure the activity of the epidermal growth factor receptor (EGFR) in tumors. ODS-2004436 labeled with the radioactive isotope fluorine-18 shows significantly higher uptake in the xenograft models of lung cancer with EGFR mutations compared to the wild-type models, and could be used to distinguish the mutation status. ODS-2004436 can be used to identify EGFR-positive tumors and predict their response to certain reagent treatments, especially for non-small cell lung cancer (NSCLC) .
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-
- HY-161857
-
|
|
Akt
mTOR
Caspase
CDK
|
Cancer
|
|
Akt/mTOR-IN-1 (Compound 8r) is an AKT/mTOR signaling pathway inhibitor exhibiting an IC50 value of 0.8 µM with anticancer activity. Akt/mTOR-IN-1 can decrease the expression of Caspase 3 and increase the expression of the autophagic protein Cyclin B1, thereby inducing cell autophagy and apoptosis. Akt/mTOR-IN-1 can be used in research related to non-small cell lung cancer (NSCLC) .
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-
- HY-114277
-
Sotorasib
Maximum Cited Publications
109 Publications Verification
AMG-510
|
Ras
|
Cancer
|
|
Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
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-
- HY-179418
-
|
|
Apoptosis
|
Cancer
|
|
Ceritinib-platinum(IV)-4-phenylbutyrate (complex 7) is a Ceritinib (HY-15656)-conjugated Platinum(IV) prodrug with anticancer activity. Ceritinib-platinum(IV)-4-phenylbutyrate induces S-phase arrest, DNA damage responses, and apoptosis. Ceritinib-platinum(IV)-4-phenylbutyrate combines cytotoxicity with immune and anti-invasive activation in cancer cell models. Ceritinib-platinum(IV)-4-phenylbutyrate can be used for cancer research, such as non-small cell lung cancer (NSCLC) .
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-
- HY-10261A
-
|
BIBW 2992MA2
|
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
|
Cancer
|
|
Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
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-
- HY-10261
-
|
BIBW 2992
|
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
|
Cancer
|
|
Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
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-
- HY-10261D
-
|
BIBW 2992 oxalate
|
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
|
Cancer
|
|
Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
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-
- HY-180430
-
|
|
Drug Derivative
|
Cancer
|
|
Antitumor agent-208, a Bufalin (HY-N0877) analogue, is a potent and orally active antitumor agent. Antitumor agent-208 exhibits antiproliferative activity against tumor cell line (IC50 =0.30-1.09 nM). Antitumor agent-208 inhibits tumor growth in a MV-4-11 xenograft mouse model. Antitumor agent-208 can be used for cancer research, such as acute myeloid leukemia (AML) and non-small cell lung cancer (NSCLC) .
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-
- HY-P991628
-
|
PF-08634404
|
PD-1/PD-L1
VEGFR
|
Cancer
|
|
SSGJ-707 (PF-08634404) is a bispecific antibody targeting VEGF and PD-1. SSGJ-707 exerts dual anti-tumor effects by neutralizing VEGF and blocking the PD-1 signaling pathway. SSGJ-707 can be combined with platinum-based chemotherapy to inhibit advanced non-small cell lung cancer (NSCLC), and its inhibitory effect is not limited by PD-L1 expression levels. In the HARMONi-2 trial, the objective response rate of SSGJ-707 correlates with the PD-L1 tumor proportion score, and the incidence of grade ≥3 adverse events is comparable to that of Inetetamab (HY-P99969). SSGJ-707 is being extensively investigated for a variety of malignancies including advanced NSCLC, colorectal cancer and small cell lung cancer .
|
-
- HY-179385
-
|
|
Microtubule/Tubulin
Phosphatase
Apoptosis
|
Cancer
|
|
Tubulin-IN-62 is a tubulin inhibitor targeting the colchicine-binding site. Tubulin-IN-62 exhibits IC50 values of 17.2 nM and 19.3 nM against SKOV3 and HCC827 cells, respectively. Tubulin-IN-62 inhibits microtubule polymerization, arrests the cell cycle at the G2/M phase, and induces apoptosis. Tubulin-IN-62 demonstrates significant antitumor efficacy in vivo with good tolerability. Tubulin-IN-62 can be used in ovarian cancer and non-small cell lung cancer (NSCLC) research .
|
-
- HY-159190
-
|
|
MAPKAPK2 (MK2)
|
Cancer
|
|
HRX-0233 is a small-molecule MAP2K4 inhibitor. HRX-0233 results in strong tumor shrinkage without any apparent toxicity in H358 KRASG12C-mutant non-small cell lung cancers (NSCLC) in vivo. HRX-0233 efficiently prevents feedback activation of receptor tyrosine kinases (RTKs) upon monotherapy KRAS inhibitor Sotorasib (HY-114277) and causes a more sustained and complete inhibition of MAPK signaling. HRX-0233 is promising for research of AR-negative prostate cancer, lung and colon cancers .
|
-
- HY-126830
-
|
|
Antifolate
Apoptosis
|
Cancer
|
|
Antifolate C2 is an anti-folate compound that has inhibitory effects on the proliferation of non-squamous non-small cell lung cancer (NS-NSCLC). Antifolate C2 achieves tumor selectivity by targeting proton-coupled folate transporter (PCFT), which is more selective to PCFT than the commonly used anti-folate drug Pemetrexed (HY-10820). Antifolate C2 blocks the biosynthesis of deoxypurine nucleotides by inhibiting glycinamide ribonucleotide formyltransferase (GARFTase), ultimately inhibiting the proliferation of tumor cells. Antifolate C2 can be used in studies of NS-NSCLC, especially in patients who do not respond well to Pemetrexed .
|
-
- HY-180241
-
|
|
Glutaminase
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Glutaminase C-IN-3 is a potent allosteric inhibitor of Glutaminase C (GAC) with an EC50 of 116 nM. Glutaminase C-IN-3 regulates cellular metabolites and increases reactive oxygen species (ROS) production by blocking glutamine metabolism. Glutaminase C-IN-3 exhibits strong antitumor activity in an A549 xenograft mouse model. Glutaminase C-IN-3 can be used for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-173520
-
|
|
EGFR
HDAC
|
Cancer
|
|
EGFR/HDAC-IN-1 (Compound 22c2) is a potent dual inhibitor of epidermal growth factor receptor (EGFR) and histone deacetylase (HDAC) with IC50 values of 4.81 nM, 119.4 nM and 354.8 nM for EGFR, HDAC1 and HDAC3, respectively. EGFR/HDAC-IN-1 blocks the EGFR signaling pathway and affects the histone acetylation status, thereby inhibiting tumor cell proliferation. EGFR/HDAC-IN-1 is promising for research of non-small cell lung cancer (NSCLC) .
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-
- HY-156671B
-
|
|
Ras
PI3K
ERK
mTOR
Apoptosis
|
Cancer
|
|
RMC-4998 TFA is an orally active inhibitor targeting the active or GTP-bound state of the KRAS G12C mutant. RMC-4998 TFA can form a ternary complex with intracellular CYPA and the activated KRAS G12C mutant, with an IC50 value of 28 nM. RMC-4998 TFA can inhibit ERK signaling in KRAS G12C mutant cancer cells and induce apoptosis. RMC-4998 TFA can be used for for non-small cell lung cancer (NSCLC) research .
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-
- HY-156671A
-
|
|
Ras
PI3K
ERK
mTOR
Apoptosis
|
Cancer
|
|
RMC-4998 formic is an orally active inhibitor targeting the active or GTP-bound state of the KRAS G12C mutant. RMC-4998 formic can form a ternary complex with intracellular CYPA and the activated KRAS G12C mutant, with an IC50 value of 28 nM. RMC-4998 formic can inhibit ERK signaling in KRAS G12C mutant cancer cells and induce apoptosis. RMC-4998 formic can be used for non-small cell lung cancer (NSCLC) research .
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-
- HY-10261R
-
|
BIBW 2992 (Standard)
|
Reference Standards
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
|
Cancer
|
|
Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-116749
-
|
BBSKE
|
TrxR
|
Cancer
|
|
Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC50s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR .
|
-
- HY-178824
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-180 (Compound L15) is an EGFR inhibitor. EGFR-IN-180 shows inhibitory activity against EFGR and EGFR harboring the L858R/T790M/C797S triple drug-resistant mutation, with IC50 values of 80.96 nM and 16.43 nM, reapectively. EGFR-IN-180 can be used for the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-145433
-
|
|
17β-HSD
|
Cancer
|
|
17β-HSD1-IN-1 (Compound 1) is a highly selective 17β-HSD1 inhibitor with IC50s of 5.6 and 3155 nM for 17β-HSD1 and 17β-HSD2, respectively. 17β-HSD1-IN-1 can be used for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-P991738
-
|
|
PD-1/PD-L1
VEGFR
|
Cancer
|
|
LM-299 is a PD-1/VEGF bispecific antibody. LM-299 achieves its dual binding activity through the effective binding of the anti-VEGF-A antibody at the fab end to human VEGF-A, coupled with the blockade of the PD-1/PD-L1 pathway by the anti-PD-1 antibody at the-Fc end. LM-299 can be used for the study of non-small cell lung cancer (NSCLC).
|
-
- HY-141601
-
|
ABBV-399
|
Antibody-Drug Conjugates (ADCs)
c-Met/HGFR
Microtubule/Tubulin
|
Cancer
|
|
Telisotuzumab vedotin (ABBV-399) (Teliso-V) is an anti-c-Met antibody-drug conjugate. Telisotuzumab vedotin consists of an anti-c-Met monoclonal antibody Telisotuzumab (ABT-700) (HY-P99391) and Monomethyl Auristatin E (HY-15162). Telisotuzumab vedotin exerts antitumor activity with acceptable toxicity in vivo. Telisotuzumab vedotin can be used for non-small cell lung cancer (NSCLC) research .
|
-
- HY-172392
-
|
|
MNK
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
HSND80 (Compound 1) is an orally active inhibitor of MNK/p70S6K, with Kd values of 44 nM against MNK1 and 4 nM against MNK2. HSND80 has a longer target residence time of 45 mins and 58 mins against MNK1 and MNK2 respectively. HSND80 can suppress non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppress Triple-Negative Breast Cancer (TNBC) in vitro .
|
-
- HY-178008
-
|
|
Bcl-2 Family
Caspase
Apoptosis
|
Cancer
|
|
Mcl-1-IN-16 is an effective macrocyclic myeloid cell leukemia 1 (Mcl-1) inhibitor with a Ki of below 0.08 nM. Mcl-1-IN-16 maintains high selectivity (>50,000-fold) for Mcl-1 over other antiapoptotic Bcl-2 family members Bcl-2 and Bcl-xL. Mcl-1-IN-16 leads to the activation of caspase-3/7, thereby initiating cell apoptosis. Mcl-1-IN-16 achieves tumor regression in a lung cancer-derived tumor xenograft mice model. Mcl-1-IN-16 can be used in the research of solid tumor such as nonsmall cell lung cancer (NSCLC) .
|
-
- HY-173493
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
Akt
mTOR
|
Cancer
|
|
ALK-IN-31 (Compound Ld-10) is an orally active ALK inhibitor (IC50: 1135 nM). ALK-IN-31 exhibits excellent antiproliferative activity against lung cancer H2228 cells with an IC50 value of 1.35 μM. ALK-IN-31 induces apoptosis and arrests cell proliferation in the G0/G1 phase by affecting mitochondrial function. ALK-IN-31 exerts its anti-tumor effect by downregulating the expression of p-AKT and p-mTOR in the PI3K-AKT-mTOR signaling pathway downstream of ALK. ALK-IN-31 can be used in the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-P2989
-
|
|
Endogenous Metabolite
|
Metabolic Disease
Cancer
|
|
Pyruvate carboxylase is a key mitochondrial anaplerotic enzyme that catalyzes the conversion of pyruvate to oxaloacetate. Pyruvate carboxylase not only maintains tricarboxylic acid cycle activity and redox homeostasis, but also drives hepatic gluconeogenesis and fatty acid synthesis. The activity of Pyruvate carboxylase is upregulated in insulin-resistant states, exacerbating hepatic glucose production. Pyruvate carboxylase also shows significantly enhanced expression in early-stage non-small cell lung cancer (NSCLC). Pyruvate carboxylase promotes tumor proliferation by supporting nucleotide and lipid synthesis, and its functional deficiency cannot be compensated by glutaminolysis. Pyruvate carboxylase can be used in the research of prediabetes type 2 and NSCLC .
|
-
- HY-103702
-
|
|
Proton Pump
DNA/RNA Synthesis
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
TIP48/49-IN-1 is an orally active, specific RUVBL1/2 (TIP48/49) ATPase inhibitor with an IC50 of 59 nM against purified RUVBL1/2. TIP48/49-IN-1 inhibits the DNA replication process, leading to S-phase arrest. TIP48/49-IN-1 induces apoptosis. TIP48/49-IN-1 can be used for the research of non-small cell lung cancer (NSCLC) cells .
|
-
- HY-10261AR
-
|
BIBW 2992MA2 (Standard)
|
Reference Standards
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
|
Cancer
|
|
Afatinib (dimaleate) (Standard) is the analytical standard of Afatinib (dimaleate). This product is intended for research and analytical applications. Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-121537R
-
|
|
COX
Akt
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
CAY10404 (Standard) is the analytical standard of CAY10404. This product is intended for research and analytical applications. CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities .
|
-
- HY-12965B
-
|
|
TAM Receptor
|
Cancer
|
|
(Z)-S49076 hydrochloride is an orally active inhibitor of MET and AXL that blocks the downstream signaling of these receptors both in vitro and in vivo, inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. (Z)-S49076 hydrochloride is capable of overcoming the resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) due to MET amplification in Erlotinib (HY-50896)-resistant cell lines both in vitro and in vivo. (Z)-S49076 hydrochloride can be used for research in non-small cell lung cancer (NSCLC) .
|
-
- HY-180562
-
|
|
Ras
|
Cancer
|
|
KARS-IN-1 (152) is a AKR1C3 dependent KARS inhibitor with an AC50 of 9.1 nM for human KARS. KARS-IN-1 shows anti-proliferative activity in H460 (NRF2 pathway mutant cell line with high AKR1C3 expression) and Hara (NRF2 pathway wild type cell line with low AKR1C3 expression), with AC50 values ??of 21 nM and 16 nM, respectively. KARS-IN-1 can be used for the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-177439
-
|
|
Antibody-Drug Conjugates (ADCs)
PD-1/PD-L1
|
Cancer
|
|
HLX43 is an antibody-drug conjugate (ADC) targeting PD-L1. HLX43 consists of a human monoclonal antibody anti-PD-L1 antibody Opucolimab (HY-P99785) with the drug-linker conjugate being DL-01 (HY-155870A). HLX43 exerts superior anticancer efficacy with safety profile in vivo. HLX43 can be used for non-small cell lung cancer (NSCLC), head and neck squamous cell carcinoma (HNSCC), esophageal squamous cell carcinoma (ESCC), melanoma (MEL), ovarian cancer (Ovc) research .
|
-
- HY-D1063
-
|
|
Fluorescent Dye
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
IR-780 is a near-infrared fluorescent probe for in vivo imaging of tumor cells. IR-780 is transported into tumor cells via OATPs and ABCB10, with uptake dependent on glycolytic activity and plasma membrane potential. IR-780 preferentially accumulates in tumor cell mitochondria, including those of drug-resistant cancer cells, without chemical conjugation. IR-780 generates reactive oxygen species (ROS), induces hyperthermia and apoptosis, inhibits tumor growth and recurrence, and modulates HSP70 expression upon ultrasound or 808 nm laser exposure. IR-780 acts as a sonosensitizer, photodynamic and photothermal agent, and drug delivery carrier, with low acute imaging-dose toxicity and rapid vital organ clearance. IR-780 can be used for the research of cancer, such as breast cancer, lung cancer, and non-small cell lung cancer (NSCLC) .
|
-
- HY-146194
-
|
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
NHEJ inhibitor-1 (Compound C2) is a trifunctional Pt(II) complex, alleviates the non-homologous end connection (NHEJ)/homologous recombination (HR)-related double strand breaks (DSBs) repairs to evade Cisplatin-resistance in non-small cell lung cancer (NSCLC). NHEJ inhibitor-1 inhibits the damage repair proteins Ku70 and Rad51 to make tumors re-sensitive to Cisplatin. NHEJ inhibitor-1 also induces ROS generation and MMP deduction .
|
-
- HY-149695
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
|
-
- HY-119307R
-
|
TMI-005 (Standard)
|
MMP
TNF Receptor
Reference Standards
|
Cancer
|
|
Apratastat (Standard) is the analytical standard of Apratastat. This product is intended for research and analytical applications. Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC) . Apratastat is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-114277R
-
|
AMG-510 (Standard)
|
Ras
Reference Standards
|
Cancer
|
|
Sotorasib (Standard) is the analytical standard of Sotorasib. This product is intended for research and analytical applications. Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
|
-
- HY-14463
-
|
AT13387
|
HSP
|
Cancer
|
|
Onalespib (AT13387) is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor. Onalespib inhibits the proliferation, survival and migration. Onalespib decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib shows antitumor activity. Onalespib has the potential for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-105369
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
KF-20444 is an orally active ALK inhibitor with blood-brain barrier penetration. KF-20444 exhibits strong inhibitory activity against ALK fusion proteins (EML4-ALK) and ALK resistance mutations (including L1196M, G1202R, and F1174L). KF-20444 effectively suppresses the phosphorylation of ALK in ALK-driven cancer cell lines, thereby inhibiting cancer cell proliferation and inducing apoptosis. KF-20444 demonstrates anti-tumor efficacy in mouse models bearing ALK-positive non-small cell lung cancer (NSCLC) or neuroblastoma. KF-20444 can be used for the study of ALK-driven malignancies .
|
-
- HY-P99117
-
|
AK104
|
PD-1/PD-L1
CTLA-4
|
Inflammation/Immunology
Cancer
|
|
Cadonilimab (AK104) is a humanized tetravalent IgG1 bispecific antibody targeting PD1/CTLA4. Cadonilimab blocks both PD-1 and CTLA-4 pathways, thereby relieving their corresponding immunosuppressive effects and reversing tumor specific T cell exhaustion. Cadonilimab significantly downregulates Fc-mediated effector functions, including antibody-dependent cell-mediated cytotoxicity (ADCC), antibody-dependent cellular phagocytosis (ADCP), complement dependent cytotoxicity (CDC). Cadonilimab can be used for research of metastatic cervical cancer, as well as other malignancies such as gastric cancer, GEJ adenocarcinoma and non-small cell lung cancer (NSCLC) .
|
-
- HY-173268
-
|
|
TAM Receptor
|
Cardiovascular Disease
Cancer
|
|
UNC9426 is a potent and selective TYRO3 inhibitor (IC50 = 2.1 nM), demonstrating 276-fold and 90-fold selectivity over MERTK and AXL, respectively. UNC9426 reduces platelet aggregation without increasing bleeding time and blocks TYRO3-dependent functions in tumor cells and macrophages. UNC9426 demonstrates a favorable safety profile with no significant increase in bleeding risk in vivo. UNC9426 can be used for functional studies of TYRO3-dependent phenotypes such as non-small cell lung cancer (NSCLC) .
|
-
- HY-P990947
-
|
AZD9592 Antibody
|
ADC Antibody
EGFR
|
Cancer
|
|
Tilatamig (AZD9592 Antibody) is a human antibody of the Ig (G1-κ_G1-λ2) subtype that targets EGFR/MET. Tilatamig conjugates with the Top1 inhibitor AZ14170133 (HY-145399) to form the antibody-drug conjugate (ADC) Tilatamig samrotecan (HY-171124) (AZD9592). Tilatamig accurately targets NSCLC models including EGFR-mutant, EGFR-wildtype, and EGFR tyrosine kinase inhibitor-treated ones, and its activity correlates with high expression of EGFR, c-MET and SLFN11. Tilatamig is available for in vivo anti-tumor studies in patient-derived xenograft models of non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) .
|
-
- HY-10261E
-
|
(R)-BIBW 2992
|
EGFR
c-Met/HGFR
p38 MAPK
|
Cancer
|
|
(R)-Afatinib ((R)-BIBW 2992) is the Afatinib isomer. Afatinib (HY-10261) is an orally active, potent and irreversible dual specificity inhibitor of?ErbB?family (EGFR?and?HER2), with?IC50?values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for?EGFR wt, EGFR L858R,?EGFR L858R/T790M?and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung?cancer?(NSCLC) and gastric?cancer .
|
-
- HY-170665
-
|
|
EGFR
|
Cancer
|
|
EGFR T790M/L858R-IN-9 (Compound 8) is an EGFR-L858R/T790M inhibitor that demonstrates potent inhibitory phosphorylation effects against the EGFR-L858R/T790M mutant kinase, with an IC50 value of 0.0064µM. EGFR T790M/L858R-IN-9 also inhibits the proliferation of non-small cell lung cancer (NSCLC) cells and can be utilized in cancer research .
|
-
- HY-181087
-
|
|
PERK
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Caspase
Bcl-2 Family
|
Cancer
|
|
Anticancer agent 296 is a potent anticancer agent that activates the PERK-eIF2α-CHOP signaling pathway to induce endoplasmic reticulum stress, thereby regulating caspase and Bcl-2 family proteins, ultimately leading to apoptosis. Anticancer agent 296 increases intracellular levels of reactive oxygen species (ROS), reduces mitochondrial membrane potential, and promotes Ca 2+ release. Anticancer agent 296 suppresses cell colony formation and S-phase cell proliferation, and induces autophagy. Anticancer agent 296 is applicable for research on non-small cell lung cancer (NSCLC) .
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- HY-17654
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EGFR
mTOR
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Cancer
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BIEGi-1 is an EGFR inhibitor. BIEGi-1 effectively disrupts the EGFR-Rheb interaction in cells. BIEGi-1 robustly inhibits EGFR kinase activity (reduces p-Y1068-EGFR) as well as mTORC1 activation (reduces p-T389-S6K1) in EGFR-mutant cells. BIEGi-1 shows strong antiproliferative effects on EGFR-mutant PC9 and HCC827 cells with IC50 values of 17 nM and 20 nM, respectively. BIEGi-1 can be used for the study of cancers harboring EGFR mutations, such as non-small cell lung cancer (NSCLC) .
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- HY-P99157
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CD276/B7-H3
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Cancer
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Omburtamab is a humanized monoclonal antibody targeting B7-H3 (CD276). Omburtamab selectively binds to B7-H3 highly expressed on the surface of tumor cells and activates anti-tumor immune responses mediated by T cells and natural killer (NK) cells. Omburtamab can promote the specific infiltration of CAR-T cells into tumors, enhance the killing function of NK cells through the CD16 signaling pathway, and regulate tumor cell glucose metabolism (such as inhibiting the Warburg effect). Omburtamab has the potential to inhibit solid tumors such as non-small cell lung cancer (NSCLC) .
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- HY-114277S
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AMG-510-d7
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Isotope-Labeled Compounds
Ras
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Cancer
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Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
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- HY-P10978
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PD-1/PD-L1
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Cancer
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NK224 is a peptide-based radiotracer targeting human PD-L1, with dual-radionuclide ( 68Ga and 18F) labeling compatibility enabled by the NOTA chelator. NK224 exhibits high binding affinity to PD-L1, with an IC50 value of 2.45 nM. NK224 visualizes intrapatient tumor heterogeneity and dynamically monitors PD-L1 target occupancy during immunotherapy. NK224 can be used for the study of non-small cell lung cancer (NSCLC) .
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- HY-114277S2
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AMG-510-d3
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Isotope-Labeled Compounds
Ras
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Cancer
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Sotorasib-d3 (AMG-510-d3) is deuterium labeled Sotorasib. Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C?mutated locally advanced or metastatic non?small cell lung cancer (NSCLC) .
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- HY-153268
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BDTX-1535; EGFR-IN-76
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EGFR
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Infection
Neurological Disease
Metabolic Disease
Cancer
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Silevertinib (BDTX-1535) is an irreversible, brain-penetrant, selective and orally active EGFR inhibitor with wild-type EGFR-sparing. Silevertinib targets key EGFR resistance mutations, including the kinase domain (C797S, L718Q, G724S, S768I), extracellular domain (EGFRvIII, A289X), and EGFR amplification. Silevertinib exerts anti-tumor activity with well tolerated in vivo. Silevertinib can be used for non-small cell lung cancer (NSCLC) and glioblastoma (GBM) research .
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- HY-179522
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EGFR
Apoptosis
Bcl-2 Family
Caspase
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Cancer
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EGFR-IN-186 is a potent inhibitor of EGFR with an IC50 of 0.065 µM. EGFR-IN-186 also exhibits inhibitory activity against EGFR L858R (IC50 = 0.528 µM) and EGFR T790M (IC50 = 0.465 µM). EGFR-IN-186 induces apoptosis by increasing Bax and caspase-3 levels and down-regulating Bcl-2 expression level. EGFR-IN-186 can be used for the research of non-small cell lung cancer (NSCLC) .
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- HY-175864
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EGFR
Apoptosis
p38 MAPK
ERK
Akt
STAT
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Inflammation/Immunology
Cancer
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EGFR-IN-173 is an orally active, pan-mutant EGFR tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR 19del/T790M/C797S with an IC50 of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC50 = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research .
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- HY-121246
-
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AKF-PD
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ACSL Family
NF-κB
ERK
TGF-beta/Smad
|
Inflammation/Immunology
Cancer
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Fluorofenidone (AKF-PD) is an orally active compound with anti-fibrotic, antioxidant, and anti-inflammatory pharmacological effects. Fluorofenidone downregulates the expression of ACSL4, upregulates GPX4 expression and inhibits the NF-κB signaling pathway to alleviate inflammation and fibrosis. Fluorofenidone ameliorates cholestasis and fibrosis by inhibiting hepatic Erk/-Egr-1 signaling and Tgfβ1/Smad pathway in mice. Fluorofenidone demonstrates protective effects against chronic lung injury in mice. Fluorofenidone can be used for the study of chronic obstructive pulmonary disease (COPD), pulmonary interstitial fibrosis (PIF) and non-small cell lung cancer (NSCLC) .
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- HY-113916
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AT13387 lactate
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HSP
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Cancer
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Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an Kd value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC) .
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- HY-178451
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|
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Apoptosis
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Cancer
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NQO1-responsive prodrug is a prodrug of Gemcitabine (dFdC) (HY-17026) with anti-cancer effect. NQO1-responsive prodrug remains stable in plasma and liver/intestinal S9 fractions, releasing dFdC in an NQO1-dependent manner. NQO1-responsive prodrug induces S-phase arrest and apoptosis. NQO1-responsive prodrug inhibits tumor growth in an A549 xenograft mouse model. NQO1-responsive prodrug can be used for breast and non-small cell lung cancer (NSCLC) research .
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-
- HY-164476
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EGFR
GSK-3
PD-1/PD-L1
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Cancer
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|
ES-072 is an orally effective selective EGFR mutant (EGFR-T790M) inhibitor. ES-072 activates GSK3α by inhibiting EGFR-T790M activity, which promotes phosphorylation of PD-L1 at Ser279 and Ser283. The phosphorylated PD-L1 recruits the E3 ubiquitin ligase ARIH1, leading to ubiquitination and proteasomal degradation of PD-L1. This mechanism not only reduces cancer cell growth but also enhances anti-tumor immune response by lowering PD-L1 levels. ES-072 can be used to inhibit proliferation in non-small cell lung cancer (NSCLC) cells .
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- HY-176942
-
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ROS1-IN-3
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ROS Kinase
Trk Receptor
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Cancer
|
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YP0322 (ROS1-IN-3) is a potent orally active, selective, and CNS-penetrant ROS1 inhibitor. JYP0322 selectively inhibits human wild-type ROS1 and human ROS1 G2032R with IC50s of 0.37 and 0.3 nM, respectively, showing 6-130-fold selectivity over TRKA, TRKB, and TRKC. JYP0322 inhibits proliferation of ROS1 fusion-expressing cells, and inhibits tumor growth in mouse xenograft models. JYP0322 can be used for the research of non-small cell lung cancer (NSCLC) .
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- HY-147858A
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PROTACs
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Cancer
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PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13 .2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC50 of 46 .82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research .
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- HY-E70717
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FGFR
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Cancer
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FGFR1 has been implicated in numerous cancer types including non-small cell lung cancer (NSCLC). FGFR1 is activated upon FGF binding to its extracellular domain, resulting in protein dimerization and transautophosphorylation of the intracellular tyrosine kinase domains. FGFR1 V561M gatekeeper mutation drives Fexagratinib (AZD4547) (HY-13330) resistance through STAT3 Activation and EMT. FGFR1 V561M Recombinant Human Active Protein Kinase is a recombinant FGFR1 V561M protein that can be used to study FGFR1 V561M-related functions .
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- HY-178939
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EGFR
Akt
PERK
Apoptosis
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Neurological Disease
Cancer
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EGFR-IN-181 is an orally active, potent, brain-penetrant EGFRL858R/T790M/C797S triple mutations inhibitor (IC50 = 1.32 nM). EGFR-IN-181 can inhibit EGFR phosphorylation (p-EGFR) and phosphorylation of its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK). EGFR-IN-181 can induce apoptosis and cause G2 phase arrest. EGFR-IN-181 can be used for the study of non-small cell lung cancer (NSCLC) and brain metastases .
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-
- HY-161269
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EGFR
|
Cancer
|
|
EGFR-IN-101 (I-10) is a 2-phenylamino pyrimidine derivative. EGFR-IN-101 is a EGFR inhibitor. The IC50 values for EGFR L858R/T790M/C797S and Ba/F3-EGFR L858R/T790M/C797S are 33.26 and 106.4 nM, respectively. EGFR-IN-101 can be used IN the study of non-small cell lung cancer (NSCLC) .
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- HY-N7694
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TGF-β Receptor
JAK
STAT
Apoptosis
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Inflammation/Immunology
Cancer
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Isotoosendanin is an orally active TGFβR1 inhibitor and abrogating its kinase activity (IC50 = 6732 nM). Isotoosendanin inhibits the JAK/STAT3 signaling pathway by directly targeting SHP-2, enhancing its stability, and reducing its ubiquitination. Isotoosendanin inhibits TGF-β-induced reduces the migration, invasion, and metastasis in triple-negative breast cancer (TNBC) cells. Isotoosendanin exhibits anti-tumor efficacy in TNBC xenograft models and A549 xenograft tumors. Isotoosendanin exhibits significant anti-inflammatory effects in acetic acid-induced vascular permeability and λ-carrageenan-induced hind paw edema tests. Isotoosendanin can be used for the study of non-small cell lung cancer (NSCLC), TNBC and inflammation .
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-
- HY-101522
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EGFR
BMX Kinase
Btk
MEK
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Cancer
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CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ～10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines .
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- HY-121246R
-
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ACSL Family
Reference Standards
NF-κB
ERK
TGF-beta/Smad
|
Inflammation/Immunology
|
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Fluorofenidone (Standard) is the analytical standard of Fluorofenidone (AKF-PD) (HY-121246). This product is intended for research and analytical applications. Fluorofenidone is an orally active compound with anti-fibrotic, antioxidant, and anti-inflammatory pharmacological effects. Fluorofenidone downregulates the expression of ACSL4, upregulates GPX4 expression and inhibits the NF-κB signaling pathway to alleviate inflammation and fibrosis. Fluorofenidone ameliorates cholestasis and fibrosis by inhibiting hepatic Erk/-Egr-1 signaling and Tgfβ1/Smad pathway in mice. Fluorofenidone demonstrates protective effects against chronic lung injury in mice. Fluorofenidone can be used for the study of chronic obstructive pulmonary disease (COPD), pulmonary interstitial fibrosis (PIF) and non-small cell lung cancer (NSCLC) .
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-
- HY-134877
-
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EGFR
ERK
Akt
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Cancer
|
|
BAY 2476568 is a potent and mutant-selective inhibitor targeting EGFR exon20 insertion variants. BAY 2476568 potently inhibits the kinase activity of EGFR exon20 insertion mutants (insASV, insSVD, insNPG) with IC50 values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 inhibits EGFR (Y1068) phosphorylation and reduces the phosphorylation of ERK1/2 and Akt (S473) in Ba/F3 cells expressing EGFR exon20 insertion mutants (insASV, insSVD). BAY 2476568 can be used for the study of non-small cell lung cancer (NSCLC) driven by EGFR exon20 insertion mutations .
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-
- HY-173237
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|
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CDK
Epigenetic Reader Domain
|
Cancer
|
CDK4/6/BRD4-IN-1 (B15) is an inhibitor of CDK4, CDK6 and BRD4, with IC50 values of 220 nM, 146 nM, 106 nM and 85 nM for BRD4-BD2, BRD4-BD1, CDK6 and CDK4, respectively. CDK4/6/BRD4-IN-1 (B15) can be used in the study of NSCLC (Non-Small Cell Lung Cancer). CDK4/6/BRD4-IN-1 (B15) induces cell cycle arrest and apoptosis .
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-
- HY-178391
-
|
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ROS Kinase
p38 MAPK
ERK
Apoptosis
|
Cancer
|
|
SMU-037 is an orally active and selective ROS1 inhibitor that demonstrates potent activity (IC₅₀ = 6.8 nM) and possesses the ability to penetrate the blood-brain barrier. SMU-037 shows ~25-fold selectivity over ALK, and superior sensitivity against the G2032R mutation. SMU-037 attenuates phosphorylation of ROS1 and downstream MAPK-ERK signaling pathway, leading to cell cycle arrest and apoptosis. SMU-037 effectively suppresses tumor progression in both xenograft and intracranial mouse models. SMU-037 can be used for non-small cell lung cancer (NSCLC) research .
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-
- HY-180965
-
|
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PROTACs
Anaplastic lymphoma kinase (ALK)
EGFR
Apoptosis
|
Cancer
|
|
Pro-PEG3-BA is an EML4-ALK/EGFR PROTAC degrader, degrading EML4 ALK and EGFR mutant (L858R/T790M) with DC 50 values of 0.42 and 13.50 μM, respectively. Pro-PEG3-BA hinders proliferation and induces cell cycle arrest and apoptosis of NSCLC cells in vitro. Pro-PEG3-BA shows safety profile and decreases EML4-ALK protein via rewiring the ubiquitin- proteasome system in vivo. Pro-PEG3-BA can be used for non-small cell lung cancer research .
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- HY-174088
-
|
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CDK
Discoidin Domain Receptor
Apoptosis
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
|
Cancer
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|
CDK4/6/BRD4-IN-2 (Compound PJ2) is a dual inhibitor of CDK4/6 and BRD4 with IC50 values for CDK4, CDK6, BRD4 (BD1), and BRD4 (BD2) of 168.75, 292.45, 23.17, and 3.12 nM respectively. CDK4/6/BRD4-IN-2 has a strong inhibitory effect on non-small cell lung cancer (NSCLC) cell lines. CDK4/6/BRD4-IN-2 induces cell cycle arrest, senescence and apoptosis through ROS-mediated DNA damage. CDK4/6/BRD4-IN-2 can also effectively inhibit the migration and invasion of NCI-H358 cells. CDK4/6-IN-2 can be used for the study of KRAS-mutated NSCLC .
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-
- HY-124295
-
|
ABT-301; MPT0E028; TMU-C-0012
|
HDAC
Akt
Apoptosis
|
Inflammation/Immunology
Cancer
|
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Imofinostat (ABT-301; MPT0E028) is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. Imofinostat has a weak inhibitory effect on HDAC8 (IC50 of 2.5 μM), but no inhibitory effect on HDAC4 (IC50>10 μM). Imofinostat reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. Imofinostat has a broad-spectrum antitumor activity, including colorectal cancer, B-cell lymphoma, non-small cell lung carcinoma (NSCLC), and pancreatic cancer, while also showing therapeutic potential in non-tumor diseases like emphysema and pulmonary fibrosis .
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-
- HY-175756
-
|
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Molecular Glues
SWI/SNF Complex
|
Cancer
|
|
SMARCA2/4 degrader-1 is a SMARCA2/4 molecular glue degrader with a DCAF16 EC50 of 110 nM. SMARCA2/4 degrader-1 covalently adducts at cysteine to form a ternary complex with SMARCA2/4 and recruits CUL4 DCAF16 and CRL1 FBXO22 E3 ligase complexes. SMARCA2/4 degrader-1 induces ubiquitination and proteasomal degradation of SMARCA2/4. SMARCA2/4 degrader-1 can be used for research of SMARCA4-deficient malignancies, non-small cell lung cancer (NSCLC), and colorectal cancer .
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-
- HY-171509
-
|
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Drug-Linker Conjugates for ADC
Apoptosis
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Cancer
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|
Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27), an agent-linker conjugate for ADC, consists the ADC linker Mal-N(Me)-C6-N(Me) and a potent ADC cytotoxin PNU-159682. Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) selectively delivers the payload to CD46-expressing cells, where the linker is cleaved by cathepsin B to release PNU-159682, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 shows durable tumor regression in xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) .
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-
- HY-175206
-
|
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P-glycoprotein
|
Cancer
|
|
P-gp-IN-30 (Compound 13) is a P-glycoprotein (P-gp) inhibitor by targeting YB-1. P-gp-IN-30 significantly enhances sensitivity to Paclitaxel by reducing total YB-1 and nucleus YB-1 protein expression, inhibiting the expression and function of downstream P-gp, further suppressing the efflux rate of Paclitaxel. P-gp-IN-30 potently inhibits tumor growth in A549/Taxol xenografts mice model with combination of Paclitaxel (HY-B0015). P-gp-IN-30 can be used for non-small cell lung cancer (NSCLC) research .
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-
- HY-172920
-
|
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Wnt
β-catenin
EGFR
ERK
COX
Akt
GSK-3
c-Myc
Apoptosis
Interleukin Related
JNK
|
Inflammation/Immunology
Cancer
|
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Wnt/β-catenin-IN-6 is an orally active Wnt/β-catenin pathway inhibitor. Wnt/β-catenin-IN-6 blocks the AKT/GSK-3β/β-catenin signaling pathway, leading to reduced expression of Wnt target genes (c-Myc, c-Jun). Wnt/β-catenin-IN-6 reduces COX2 expression and IL-8 levels, highlighting its dual anti-inflammatory and antitumor effects. Wnt/β-catenin-IN-6 can induce apoptosis. Wnt/β-catenin-IN-6 serves as a tool for non-small cell lung cancer (NSCLC) research .
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-
- HY-121246S
-
|
AKF-PD-d3
|
Isotope-Labeled Compounds
ACSL Family
NF-κB
ERK
TGF-beta/Smad
|
Inflammation/Immunology
Cancer
|
|
Fluorofenidone-d3 (AKF-PD-d3) is deuterium labeled Fluorofenidone (AKF-PD) (HY-121246). Fluorofenidone is an orally active compound with anti-fibrotic, antioxidant, and anti-inflammatory pharmacological effects. Fluorofenidone downregulates the expression of ACSL4, upregulates GPX4 expression and inhibits the NF-κB signaling pathway to alleviate inflammation and fibrosis. Fluorofenidone ameliorates cholestasis and fibrosis by inhibiting hepatic Erk/-Egr-1 signaling and Tgfβ1/Smad pathway in mice. Fluorofenidone demonstrates protective effects against chronic lung injury in mice. Fluorofenidone can be used for the study of chronic obstructive pulmonary disease (COPD), pulmonary interstitial fibrosis (PIF) and non-small cell lung cancer (NSCLC) .
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-
- HY-172733S
-
|
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Isotope-Labeled Compounds
Histone Methyltransferase
|
Cancer
|
|
PRMT5-MTA-IN-3-d3 (compound P22) is the deuterium labeled PRMT5-MTA-IN-3 (HY-172733). PRMT5-MTA-IN-3-d3 is an orally active PRMT5-MTA inhibitor. PRMT5-MTA-IN-3-d3 has antiproliferative effects on HTC116-MTAP del and wild type colorectal cancer HCT-116 cell lines, with IC50 values of 6 nM and 961 nM, respectively. PRMT5-MTA-IN-3-d3 has anticancer effects, especially for MTAP-deficient tumors, such as non-small cell lung cancer (NSCLC), pancreatic cancer .
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-
- HY-171124
-
|
AZD9592
|
Antibody-Drug Conjugates (ADCs)
EGFR
c-Met/HGFR
Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
|
Tilatamig samrotecan (AZD9592) is an anti-EGFR/c-MET antibody-drug conjugate (ADC). Tilatamig samrotecan consists of an anti-EGFR/c-MET antibody with the drug-linker conjugate being AZ14170133 (HY-145399) (a topoisomerase I (TOP1i) inhibitor payload). Tilatamig samrotecan induces multiple DNA damage response pathway markers (like ATM, ATR, γH2AX). Tilatamig samrotecan selectively binds to EGFR and c-MET, delivering the cytotoxic payload. Tilatamig samrotecan exerts anti-tumor activity in vivo. Tilatamig samrotecan can be used for non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) research .
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-
- HY-157229
-
STX-721
1 Publications Verification
|
EGFR
ERK
|
Cancer
|
|
STX-721 is an orally active, irreversible, covalent EGFR exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of EGFR (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations .
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-
- HY-155721
-
|
22-4′-Pyridinecarbonyl jorunnamycin A
|
Akt
mTOR
|
Cancer
|
|
22-(4′-py)-JA is a semisynthetic derivative of junamycin A (JA) that can be isolated from the Thai blue sponge (Xestospongia sp.). 22-(4′-py)-JA has antimetastatic activity and can inhibit AKT/mTOR/p70S6K signaling. 22-(4′-py)-JA inhibits tumor cell invasion and tube formation in human umbilical vein endothelial cells (HUVEC), downregulates metalloproteinases (MMP-2 and MMP-9), hypoxia-inducible factor 1α (HIF-1α) and vascular endothelial growth factor (VEGF). 22-(4′-py)-JA has potent anticancer activity against non-small cell lung cancer (NSCLC) .
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-
- HY-147858
-
|
|
PROTACs
EGFR
Apoptosis
|
Cancer
|
|
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-174315
-
|
|
PROTACs
Anaplastic lymphoma kinase (ALK)
Akt
ERK
|
Cancer
|
|
WZH-17-002 is a WZH-15-125-based ALK PROTAC degrader with a DC50 of 25 nM. WZH-17-002 enhances activities against Lorlatinib (HY-12215)-resistant ALK compound mutations. WZH-17-002 significantly reduces drug resistance in ALK-fusion non-small cell lung cancer (NSCLC) and inhibits tumor growth in EML4-ALK G1202R/L1196 M xenograft mice model . Pink: ALK ligand (HY-174314); Blue: CRBN ligase ligand (HY-14658); Black: linker (HY-174316)
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-
- HY-W1128879
-
|
SKPer1
|
Molecular Glues
E1/E2/E3 Enzyme
|
Cancer
|
|
XMU-MP-8 (SKPer1) is a potent molecular glue degrader that targets the oncoprotein SKP2. XMU-MP-8 simultaneously binds to the F-box domain of SKP2 (Kd ≈ 36 μM) and the N-terminal TPR domain of the E3 ligase STUB1 (Kd ≈ 2.5 μM), forming a stable SKP2-SKPer1-STUB1 ternary complex (Kd ≈ 8.9 nM) that induces SKP2 ubiquitination and proteasomal degradation. XMU-MP-8 selectively eliminates SKP2-expressing cancer cells. XMU-MP-8 exhibits substantial tumour suppression with good safety profiles in vivo. XMU-MP-8 can be used for cancer research, such as non-small cell lung adenocarcinoma (NSCLC) and prostatic adenocarcinoma .
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-
- HY-181542
-
|
|
Aldose Reductase
|
Cancer
|
|
SG-55 is a selective, noncompetitive and orally active AKR1C3 inhibitor with an IC50 of 5 nM and a Ki of 10 nM. SG-55 shows >2000-fold selectivity for AKR1C3 over AKR1C1, AKR1C2, and AKR1C4 (> 10 μM). SG-55 increases the ratio of reduced/oxidized nicotinamide adenine dinucleotide phosphate (NADPH/NADP +), decreases the ratio of reduced/oxidized glutathione (GSH/GSSG), and induces DNA double-strand breaks. SG-55 can overcome Osimertinib (HY-15772) resistance mediated by EGFR C797S triple mutation in non-small cell lung cancer (NSCLC) .
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-
- HY-161275
-
|
|
EGFR
Akt
ERK
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-W018324
-
|
5hmC
|
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Cancer
|
|
5-Hydroxymethylcytosine (5hmC) is an oxidized forms of 5-methylcytosine (5mC) in mammalian DNA. 5-Hydroxymethylcytosine is produced from 5mC in an enzymatic pathway involving three 5mC oxidases, Ten-eleven translocation (TET)1, TET2, and TET3. The conversion of 5mC into 5hmC can be the first step in a pathway leading towards DNA demethylation. 5-Hydroxymethylcytosine is associated with gene transcription and frequently used as a mark to investigate dynamic DNA methylation conversion during mammalian development. 5-Hydroxymethylcytosine can be used for the study of non-small cell lung cancer (NSCLC), neurodegenerative diseases (Alzheimer’s, Parkinson’s) and hematological malignancies (acute myeloid leukemia, myelodysplastic syndromes) .
|
-
- HY-175839
-
|
|
PROTACs
EGFR
ATP Synthase
|
Cancer
|
|
PROTAC EGFR degrader 15 is a Pomalidomide (HY-10984)-based Gefitinib (HY-50895) EGFR PROTAC degrader. PROTAC EGFR degrader 15 triggers EGFR degradation via ubiquitin-proteasome-dependent proteolysis and autophagy-lysosome activation pathways. PROTAC EGFR degrader 15 targets ETFA to enhance ATP production. PROTAC EGFR degrader 15 significantly suppresses tumor growth in a Gefitinib-acquired resistant HCC-827 xenograft model. PROTAC EGFR degrader 15 can be used for the study of non-small cell lung cancer (NSCLC) (Pink: EGFR ligand (HY-W109039); Blue: CRBN ligand (HY-10984); Black: Linker (HY-W679737)) .
|
-
- HY-155358
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
Os30, a potent fourth-generation EGFR inhibitor, is a potent EGFRC797S-TK inhibitor with IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively. Os30 can suppress EGFR phosphorylation, arrest at G1 phase and induce the apoptosis of KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. Os30 shows potent antitumor efficacy on non-small cell lung cancer (NSCLC) with EGFmRC797S mutation .
|
-
- HY-180245
-
|
|
STAT
Ferroptosis
Apoptosis
Glutathione Peroxidase
Bcl-2 Family
Reactive Oxygen Species (ROS)
|
Cancer
|
|
STAT3-IN-51 is a STAT3 inhibitor that directly binds to the STAT3 SH2 domain. STAT3-IN-51 induces apoptosis, ferroptosis, and immunogenic cell death (ICD) to potentiate anti-tumor immunity. STAT3-IN-51 inhibits STAT3 activation (phosphorylation, p-STAT3) and its downstream signaling. STAT3-IN-51 induces ROS generation, decreases Bcl-2 expression, disruptes mitochondrial function, suppresses GPX4 activity, and promotes lipid peroxidation. STAT3-IN-51 can be used for the study of colorectal carcinoma, breast adenocarcinoma, non-small cell lung cancer (NSCLC) and Cisplatin (HY-17394)-resistant pulmonary adenocarcinoma .
|
-
- HY-181502
-
|
|
EGFR
ERK
PARP
Caspase
Bcl-2 Family
Apoptosis
|
Cancer
|
|
EGFR-IN-197 is an EGFR inhibitor with IC50 values of 19.5 nM and 12.0 nM against EGFR L858R/T790M and EGFR L858R/T790M/C797S, respectively. EGFR-IN-197 arrests the cell cycle of NCI-H1975 cells at the G2/M phase, while inhibiting their proliferation, colony formation and migration; it also inhibits mitochondrial translocation and upregulates mitochondrial H2S levels. EGFR-IN-197 disrupts anti-apoptotic signaling pathways by regulating apoptosis-related proteins; it induces DNA damage and activates pro-apoptotic pathways to trigger apoptosis. EGFR-IN-197 can be used in studies related to non-small cell lung cancer (NSCLC) .
|
-
- HY-175527
-
|
|
HyT
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
ALK degrader 2 is an orally active ALK HyT degrader that degrades EML4-ALK levels (DC50 = 8 nM) and nucleophosmin (NPM)-ALK protein levels (DC50 = 102 nM). ALK degrader 2 mediates ALK degradation via the Hsp70 chaperone system and ubiquitin-proteasome pathway. ALK degrader 2 induces significant S-phase cell cycle arrest and apoptosis in H3122 cells. ALK degrader 2 shows anti-tumor activity in mice bearing H3122 xenografts. ALK degrader 2 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: ALK ligand (HY-W754809), Blue: Hyt (HY-W013021), Black: Linker (HY-Y1760), ALK ligand-linker conjugate (HY-175528)) .
|
-
- HY-178057
-
|
|
EGFR
Akt
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
EGFR-IN-176 is an orally active and ATP-competitive EGFR mutant inhibitor (particularly C797S-mediated EGFR triple mutant). EGFR-IN-176 effectively inhibits subsequent AKT signaling and induces apoptosis in Ba/F3 and PC-9 cells expressing EGFR 19del/T790M/C797S and EGFR L858R/T790M/C797S. EGFR-IN-176 selectively inhibits EGFR signaling in cell lines harboring EGFR triple mutation and shows no inhibitory effect against A431 cells that express wild-type EGFR. EGFR-IN-176 can effectively inhibit the enzymatic activity of ALK (IC50 < 0.5 nM). EGFR-IN-176 can be used for the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-175836
-
|
|
Cytochrome P450
Apoptosis
|
Cancer
|
|
CYP1B1-IN-12 is a selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 6.05 nM. CYP1B1-IN-12 demonstrates remarkable selectivity, exceeding 1600-fold and 16,000-fold over CYP1A1 and CYP1A2, respectively. CYP1B1-IN-12 can enhance Paclitaxel (HY-B0015)-mediated apoptosis and restore Paclitaxel sensitivity in A549/Taxol-resistant cells. CYP1B1-IN-12 can inhibit the epithelial-mesenchymal transition process and reduce cells migration and invasion. CYP1B1-IN-12 can be used for the research of cancer, such as non-small cell lung cancer (NSCLC) .
|
-
- HY-175252
-
|
|
PROTACs
EGFR
Apoptosis
|
Cancer
|
|
PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC50 of about 2.9 nM and a Dmax of 93.1% for EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 selectively induces EGFR C797S degradation through a VHL and proteasome-dependent manner and downregulated EGFR-associated transcriptome and exhibits good selectivity over EGFR WT. PROTAC EGFR degrader 14 induces cell cycle arrest and apoptosis and significantly inhibits tumor growth. PROTAC EGFR degrader 14 can be used for the study of nonsmall cell lung cancer (NSCLC) (Pink: Target protein ligand: (HY-143337); Blue: E3 ligand (HY-125845); Black: Linker (HY-W004688)) .
|
-
- HY-162098
-
|
|
PROTACs
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056)) .
|
-
- HY-178448
-
|
|
EGFR
JAK
Ferroptosis
Apoptosis
Reactive Oxygen Species (ROS)
Cannabinoid Receptor
Glutathione Peroxidase
Caspase
|
Inflammation/Immunology
Cancer
|
|
EGFR-IN-178 is an orally active EGFR mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the EGFR enzyme, including Del19 (IC50 = 3.4 nM), L858R/T790 M (IC50 = 2.9 nM), and Del19/T790 M (IC50 = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC50 = 55.6 nM) and JAK3 (IC50 = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-174855
-
|
|
PI3K
mTOR
Apoptosis
Bcl-2 Family
MDM-2/p53
Caspase
|
Cancer
|
|
PI3K/mTOR-IN-17 is a dual PI3K and mTOR inhibitor with IC50 values of 1.21 μM (PI3K), and 0.21 μM (mTOR). PI3K/mTOR-IN-17 induces cells caspase-mediated apoptosis by arresting their growth in the G1-phase. PI3K/mTOR-IN-17 upregulates the levels of caspases-3, 7, 8, and 9, p53 expression and Bax/Bcl-2 ratio. PI3K/mTOR-IN-17 suppresses the PI3K/mTOR signaling pathway. PI3K/mTOR-IN-17 can be used for research of cancer, such as non-small cell lung cancer (NSCLC) .
|
-
- HY-130133
-
|
|
PI3K
mTOR
Akt
Apoptosis
Paraptosis
p38 MAPK
Mitochondrial Metabolism
P-glycoprotein
CDK
MMP
HIF/HIF Prolyl-Hydroxylase
VEGFR
|
Cancer
|
|
DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research .
|
-
- HY-W018324S
-
|
5hmC-13C,d2
|
Isotope-Labeled Compounds
|
Neurological Disease
|
|
5-Hydroxymethylcytosine- 13C,d2 is the 13C and deuterium labeled 5-Hydroxymethylcytosine (HY-W018324). 5-Hydroxymethylcytosine (5hmC) is an oxidized forms of 5-methylcytosine (5mC) in mammalian DNA. 5-Hydroxymethylcytosine is produced from 5mC in an enzymatic pathway involving three 5mC oxidases, Ten-eleven translocation (TET)1, TET2, and TET3. The conversion of 5mC into 5hmC can be the first step in a pathway leading towards DNA demethylation. 5-Hydroxymethylcytosine is associated with gene transcription and frequently used as a mark to investigate dynamic DNA methylation conversion during mammalian development. 5-Hydroxymethylcytosine can be used for the study of non-small cell lung cancer (NSCLC), neurodegenerative diseases (Alzheimer’s, Parkinson’s) and hematological malignancies (acute myeloid leukemia, myelodysplastic syndromes) .
|
-
-
-
HY-L075
-
|
|
2,886 compounds
|
|
Lung cancer is a major global health problem, as it is the leading cause of cancer-related deaths worldwide. Lung cancer is divided into two categories: small cell lung cancer and non-small cell lung cancer (NSCLC). Non-small cell lung cancer accounts for about 85 percent of lung cancers.
As with all cancers, lung cancer may be treated with surgery, chemotherapy, radiation therapy, targeted therapy, immunotherapy or a combination thereof. Targeted therapy is one of the most exciting developments in lung cancer medicine, especially for NSCLC. Extensive genomic characterization of NSCLC has led to the identification of molecular subtypes of NSCLC that are oncogene addicted and exquisitely sensitive to targeted therapies. These include activating mutations in epidermal growth factor receptor (EGFR) and BRAF or echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (ALK) fusions and ROS1 receptor tyrosine kinase fusions. These are important targets for target therapy.
MCE offers a unique collection of 2,886 compounds with identified and potential anti-lung cancer activity. These compounds target lung cancer’s major targets and signaling pathways. MCE anti-lung cancer compound library is a useful tool for anti-lung cancer drugs screening and other related research.
|
| Cat. No. |
Product Name |
Type |
-
- HY-141601
-
|
ABBV-399
|
Fluorescent Dyes
|
|
Telisotuzumab vedotin (ABBV-399) (Teliso-V) is an anti-c-Met antibody-drug conjugate. Telisotuzumab vedotin consists of an anti-c-Met monoclonal antibody Telisotuzumab (ABT-700) (HY-P99391) and Monomethyl Auristatin E (HY-15162). Telisotuzumab vedotin exerts antitumor activity with acceptable toxicity in vivo. Telisotuzumab vedotin can be used for non-small cell lung cancer (NSCLC) research .
|
-
- HY-D1063
-
|
|
Fluorescent Dyes
|
|
IR-780 is a near-infrared fluorescent probe for in vivo imaging of tumor cells. IR-780 is transported into tumor cells via OATPs and ABCB10, with uptake dependent on glycolytic activity and plasma membrane potential. IR-780 preferentially accumulates in tumor cell mitochondria, including those of drug-resistant cancer cells, without chemical conjugation. IR-780 generates reactive oxygen species (ROS), induces hyperthermia and apoptosis, inhibits tumor growth and recurrence, and modulates HSP70 expression upon ultrasound or 808 nm laser exposure. IR-780 acts as a sonosensitizer, photodynamic and photothermal agent, and drug delivery carrier, with low acute imaging-dose toxicity and rapid vital organ clearance. IR-780 can be used for the research of cancer, such as breast cancer, lung cancer, and non-small cell lung cancer (NSCLC) .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10944
-
|
NNS309
|
FAP
|
Inflammation/Immunology
Cancer
|
|
Unlabeled FXX489 (NNS309) is a fibroblast activation protein (FAP)-targeting ligand. Unlabeled FXX489 can be labeled with 68Ga and 177Lu and shows anticancer effects. Unlabeled FXX489 can be used for the study of pancreatic ductal adenocarcinoma (PDAC), non-small cell lung cancer (NSCLC), breast cancer (BC), and colorectal cancer (CRC) .
|
-
- HY-P5005
-
|
|
CMV
PD-1/PD-L1
|
Infection
Inflammation/Immunology
Cancer
|
|
VIPhyb is a vasoactive intestinal polypeptide (VIP) receptor antagonist. VIPhyb can inhibit VIP signaling, increase T-cell immunity and downregulate PD1. VIPhyb can inhibit cancer cell proliferation. VIPhyb can reduce inflammatory cytokine expression. VIPhyb can enhance viral clearance. VIPhyb can be used for the researches of cancer, infection and inflammation and immunology, such as non-small cell lung cancer (NSCLC), cytomegalovirus infection and colitis .
|
-
- HY-P10978
-
|
|
PD-1/PD-L1
|
Cancer
|
|
NK224 is a peptide-based radiotracer targeting human PD-L1, with dual-radionuclide ( 68Ga and 18F) labeling compatibility enabled by the NOTA chelator. NK224 exhibits high binding affinity to PD-L1, with an IC50 value of 2.45 nM. NK224 visualizes intrapatient tumor heterogeneity and dynamically monitors PD-L1 target occupancy during immunotherapy. NK224 can be used for the study of non-small cell lung cancer (NSCLC) .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P99269
-
|
BIBH 1; Anti-Human FAP Recombinant Antibody
|
FAP
|
Cancer
|
|
Sibrotuzumab (BIBH 1) is a humanized IgG1 monoclonal antibody targets fibroblast activation protein (FAP). Sibrotuzumab can be used for the research of colorectal cancer and non-small cell lung cancer (NSCLC) .
|
-
(5)
-
- HY-P99117
-
|
AK104
|
PD-1/PD-L1
CTLA-4
|
Inflammation/Immunology
Cancer
|
|
Cadonilimab (AK104) is a humanized tetravalent IgG1 bispecific antibody targeting PD1/CTLA4. Cadonilimab blocks both PD-1 and CTLA-4 pathways, thereby relieving their corresponding immunosuppressive effects and reversing tumor specific T cell exhaustion. Cadonilimab significantly downregulates Fc-mediated effector functions, including antibody-dependent cell-mediated cytotoxicity (ADCC), antibody-dependent cellular phagocytosis (ADCP), complement dependent cytotoxicity (CDC). Cadonilimab can be used for research of metastatic cervical cancer, as well as other malignancies such as gastric cancer, GEJ adenocarcinoma and non-small cell lung cancer (NSCLC) .
|
-
(5)
-
- HY-P9986
-
|
MTIG-7192A; RG-6058
|
CD28
|
Cancer
|
|
Tiragolumab is an immune checkpoint inhibitor binding to the T-cell immunoglobulin and ITIM domain (TIGIT). Tiragolumab in combination with Atezolizumab (HY-P9904) and Bevacizumab (HY-P9906) has benefit in unresectable hepatocellular carcinoma. Tiragolumab can be used to study non-small cell lung cancer (NSCLC) and melanoma .
|
-
(5)
-
- HY-P991628
-
|
PF-08634404
|
PD-1/PD-L1
VEGFR
|
Cancer
|
|
SSGJ-707 (PF-08634404) is a bispecific antibody targeting VEGF and PD-1. SSGJ-707 exerts dual anti-tumor effects by neutralizing VEGF and blocking the PD-1 signaling pathway. SSGJ-707 can be combined with platinum-based chemotherapy to inhibit advanced non-small cell lung cancer (NSCLC), and its inhibitory effect is not limited by PD-L1 expression levels. In the HARMONi-2 trial, the objective response rate of SSGJ-707 correlates with the PD-L1 tumor proportion score, and the incidence of grade ≥3 adverse events is comparable to that of Inetetamab (HY-P99969). SSGJ-707 is being extensively investigated for a variety of malignancies including advanced NSCLC, colorectal cancer and small cell lung cancer .
|
-
(5)
-
- HY-P99379
-
|
CAN04; Anti-IL-1RAP/IL-1R3 Reference Antibody (nidanilimab)
|
Interleukin Related
|
Cancer
|
|
Nidanilimab (CAN04) is a fully humanized monoclonal anti-IL1RAP antibody with a Kd value of 1.10 pM. Nidanilimab blocks IL1α and IL1β signaling and stimulates the immune system to destroy tumour cells. Nidanilimab can be used in research of non-small lung cancer (NSCLC) and pancreatic ductal adenocarcinoma (PDAC) .
|
-
(5)
-
- HY-P99202
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
Vibostolimab is an anti-TIGIT (T cell immunoglobulin and ITIM domain) monoclonal antibody. Vibostolimab shows antitumor activity, and can be used in non-small cell lung cancer (NSCLC) and melanoma research .
|
-
(5)
-
- HY-P991669
-
|
AML-01
|
Caspase
Apoptosis
|
Cancer
|
|
IGN523 is an anti-CD98 antibody (hCD98, KD = 0.55 nM). IGN523 induces antibody-dependent cell-mediated cytotoxicity (ADCC) activity, lysosomal membrane permeabilization, and inhibition of essential amino acid transport, ultimately leading to caspase-3 and caspase-7-mediated apoptosis of tumor cells. IGN523 inhibits tumor growth in multiple tumor xenograft models. IGN523 is useful in the research of non-small cell lung cancer (NSCLC), acute myeloid leukemia (AML), and other cancers. .
|
-
(5)
-
- HY-P99157
-
|
|
CD276/B7-H3
|
Cancer
|
|
Omburtamab is a humanized monoclonal antibody targeting B7-H3 (CD276). Omburtamab selectively binds to B7-H3 highly expressed on the surface of tumor cells and activates anti-tumor immune responses mediated by T cells and natural killer (NK) cells. Omburtamab can promote the specific infiltration of CAR-T cells into tumors, enhance the killing function of NK cells through the CD16 signaling pathway, and regulate tumor cell glucose metabolism (such as inhibiting the Warburg effect). Omburtamab has the potential to inhibit solid tumors such as non-small cell lung cancer (NSCLC) .
|
-
(5)
-
- HY-P99223
-
|
MEDI-575
|
PDGFR
|
Cancer
|
|
Tovetumab (MEDI-575) is an anti-PDGFRα monoclonal antibody that selectively blocks the PDGFRα signal transduction. Tovetumab can be used in the research of glioblastoma and non-small cell lung cancer (NSCLC) .
|
-
(5)
-
- HY-P99827
-
|
TSR-022; GSK4069889
|
Tim3
|
Cancer
|
|
Cobolimab (TSR-022) is an anti-TIM-3 monoclonal antibody. Cobolimab mediates the internalization of TIM3 with an IC50 value of 0.4464 nM. Cobolimab has potential application in solid tumors and non-small cell lung cancer (NSCLC) .
|
-
(5)
-
- HY-P990049
-
|
JMT-101; MRG003 Antibody
|
EGFR
|
Cancer
|
|
Becotatug (JMT-101) is a humanized IgG1 antibody targeting EGFR. Becotatug can also be conjugated to Afatinib (HY-10261) and Osimertinib (HY-15772) as a synthetic ADC. Becotatug can be used for the study of EGFR-mutated advanced non-small cell lung cancer (NSCLC) .
|
-
(5)
-
- HY-P99785
-
|
HLX20; HLX43 antibody
|
PD-1/PD-L1
ADC Antibody
|
Cancer
|
|
Opucolimab (HLX20) is an engineered anti-PD-L1 humanised IgG1 antibody. Opucolimab, when conjugated with camptothecin toxoid, yields the PD-L1-targeting ADC, HLX43 (HY-177439). HLX43 can be used for non-small cell lung cancer (NSCLC), head and neck squamous cell carcinoma (HNSCC), esophageal squamous cell carcinoma (ESCC), melanoma (MEL), ovarian cancer (Ovc) research .
|
-
(5)
-
- HY-P990947
-
|
AZD9592 Antibody
|
ADC Antibody
EGFR
|
Cancer
|
|
Tilatamig (AZD9592 Antibody) is a human antibody of the Ig (G1-κ_G1-λ2) subtype that targets EGFR/MET. Tilatamig conjugates with the Top1 inhibitor AZ14170133 (HY-145399) to form the antibody-drug conjugate (ADC) Tilatamig samrotecan (HY-171124) (AZD9592). Tilatamig accurately targets NSCLC models including EGFR-mutant, EGFR-wildtype, and EGFR tyrosine kinase inhibitor-treated ones, and its activity correlates with high expression of EGFR, c-MET and SLFN11. Tilatamig is available for in vivo anti-tumor studies in patient-derived xenograft models of non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) .
|
-
(5)
-
- HY-P99921
-
|
HuMax-AXL-ADC
|
Antibody-Drug Conjugates (ADCs)
TAM Receptor
|
Cancer
|
|
Enapotamab vedotin is an AXL-targeted antibody-drug conjugate (ADC) with inhibitory potential against high AXL expressing non-small cell lung cancer (NSCLC). Enapotamab vedotin also exhibits resistant to EGFR inhibitor such as Osimertinib (HY-15772) .
|
-
(5)
-
- HY-P991635
-
|
|
TNF Receptor
|
Cancer
|
|
PF-07329640 is a humanized monoclonal antibody inhibitor targeting TNFRSF3. PF-07329640 can be used for advanced/metastatic solid tumors like non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) research .
|
-
(5)
-
- HY-P991612
-
|
Sym024
|
CD73
|
Inflammation/Immunology
Cancer
|
|
S095024 is a humanized IgG1 monoclonal antibody inhibitor targeting CD73. S095024 can be used to study acute respiratory distress syndrome (ARDS), non-small cell lung cancer (NSCLC) and advanced solid tumor malignancies .
|
-
(5)
-
- HY-P991244
-
|
|
EGFR
|
Cancer
|
|
REGN-1400 is a humanized monoclonal antibody inhibitor targeting ErbB3. REGN-1400 reduces tumor cell proliferation by inhibiting ErbB3 and blocking related signaling pathways. REGN-1400 is promising for research of solid tumors such as non-small cell lung cancer (NSCLC), colorectal cancer (CRC), and squamous cell carcinoma of the head and neck (SCCHN) .
|
-
(5)
-
- HY-P991058
-
|
BMS-986315
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
Zimistobart (BMS-986315) is a fully human IgG1 antibody that targets NKG2A. Zimistobart can be used for the study of non-small cell lung cancer (NSCLC). The isotype control for Zimistobart can refer to Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
(5)
-
- HY-P991620
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
JS006 is a humanized IgG4κ monoclonal antibody inhibitor targeting TIGIT/CD155. JS006 can be used to study advanced and/or metastatic cancers with resistance to PD-1/PD-L1 inhibitor such as non-small cell lung cancer (NSCLC), advanced lymphoma and advanced/metastatic triple negative breast cancer (TNBC) .
|
-
(5)
-
- HY-P991738
-
|
|
PD-1/PD-L1
VEGFR
|
Cancer
|
|
LM-299 is a PD-1/VEGF bispecific antibody. LM-299 achieves its dual binding activity through the effective binding of the anti-VEGF-A antibody at the fab end to human VEGF-A, coupled with the blockade of the PD-1/PD-L1 pathway by the anti-PD-1 antibody at the-Fc end. LM-299 can be used for the study of non-small cell lung cancer (NSCLC).
|
-
(5)
-
- HY-P991883
-
|
Licartin; Metuximab; Mehuzumab
|
Apoptosis
CDK
Caspase
Bcl-2 Family
|
Cancer
|
|
Metuzumab (Licartin) is a human-mouse chimeric IgG1 monoclonal antibody targeting CD147. Metuzumab induces Apoptosis, reduces levels of Cyclin D1, full-length Caspase-3, and Bcl-2, and increases Bax expression. Metuzumab enhances the sensitivity of non-small cell lung cancer (NSCLC) cells to Gemcitabine (HY-17026). Metuzumab is applicable for research on hepatocellular carcinoma and non-small cell lung cancer [1] [2].
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-19939S
-
4 Publications Verification
|
|
VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium .
|
-
-
- HY-114277S
-
|
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Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
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- HY-114277S2
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Sotorasib-d3 (AMG-510-d3) is deuterium labeled Sotorasib. Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C?mutated locally advanced or metastatic non?small cell lung cancer (NSCLC) .
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- HY-121246S
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Fluorofenidone-d3 (AKF-PD-d3) is deuterium labeled Fluorofenidone (AKF-PD) (HY-121246). Fluorofenidone is an orally active compound with anti-fibrotic, antioxidant, and anti-inflammatory pharmacological effects. Fluorofenidone downregulates the expression of ACSL4, upregulates GPX4 expression and inhibits the NF-κB signaling pathway to alleviate inflammation and fibrosis. Fluorofenidone ameliorates cholestasis and fibrosis by inhibiting hepatic Erk/-Egr-1 signaling and Tgfβ1/Smad pathway in mice. Fluorofenidone demonstrates protective effects against chronic lung injury in mice. Fluorofenidone can be used for the study of chronic obstructive pulmonary disease (COPD), pulmonary interstitial fibrosis (PIF) and non-small cell lung cancer (NSCLC) .
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- HY-172733S
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PRMT5-MTA-IN-3-d3 (compound P22) is the deuterium labeled PRMT5-MTA-IN-3 (HY-172733). PRMT5-MTA-IN-3-d3 is an orally active PRMT5-MTA inhibitor. PRMT5-MTA-IN-3-d3 has antiproliferative effects on HTC116-MTAP del and wild type colorectal cancer HCT-116 cell lines, with IC50 values of 6 nM and 961 nM, respectively. PRMT5-MTA-IN-3-d3 has anticancer effects, especially for MTAP-deficient tumors, such as non-small cell lung cancer (NSCLC), pancreatic cancer .
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- HY-W018324S
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5-Hydroxymethylcytosine- 13C,d2 is the 13C and deuterium labeled 5-Hydroxymethylcytosine (HY-W018324). 5-Hydroxymethylcytosine (5hmC) is an oxidized forms of 5-methylcytosine (5mC) in mammalian DNA. 5-Hydroxymethylcytosine is produced from 5mC in an enzymatic pathway involving three 5mC oxidases, Ten-eleven translocation (TET)1, TET2, and TET3. The conversion of 5mC into 5hmC can be the first step in a pathway leading towards DNA demethylation. 5-Hydroxymethylcytosine is associated with gene transcription and frequently used as a mark to investigate dynamic DNA methylation conversion during mammalian development. 5-Hydroxymethylcytosine can be used for the study of non-small cell lung cancer (NSCLC), neurodegenerative diseases (Alzheimer’s, Parkinson’s) and hematological malignancies (acute myeloid leukemia, myelodysplastic syndromes) .
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- HY-112870AS
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Firmonertinib-d3 (Alflutinib-d3) mesylate is the deuterium labeled Firmonertinib mesylate (HY-112870A). Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and blood-brain barrier penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation.
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- HY-147858
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Alkynes
PROTAC Synthesis
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PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-179534
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Alkynes
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G13Ci-22 is a MRTX1133 (HY-134813) based KRAS G13C inhibitor. G13Ci-22 can be used for non-small cell lung cancer (NSCLC) research .
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