Search Result
Results for "
lung cancer xenograft models
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-156002
-
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Paluratide
|
Ras
ERK
|
Cancer
|
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LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer .
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-
-
- HY-164388
-
|
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Caspase
Apoptosis
Autophagy
Necroptosis
|
Cardiovascular Disease
Cancer
|
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Z-VAD is an irreversible, broad-spectrum pan-caspase inhibitor that can inhibit a variety of caspases including caspase-3, -6, -7, -8, -9, etc. (with a weaker inhibitory effect on caspase-2). Z-VAD can block apoptosis signaling pathways, induce autophagy and necrosis in tumor cells, and has anti-angiogenic activity. Z-VAD can enhance the sensitivity of breast cancer and lung cancer cells to radiotherapy in vitro and in vivo, and prolong the growth delay of tumor xenograft models. Z-VAD is well tolerated and is mainly used in research related to cancer radiosensitization and cell death pathway regulation .
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-
-
- HY-P99275
-
|
AMG-888; U3-1287
|
EGFR
Akt
ERK
PARP
Survivin
|
Cancer
|
|
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
|
-
-
- HY-P9964
-
|
11F8; IMC-11F8; LY3012211
|
EGFR
|
Cancer
|
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Necitumumab (11F8; IMC-11F8; LY3012211) is a human IgG monoclonal antibody directed against EGFR. Necitumumab binds to the EGF binding site of EGFR, blocks ligand binding, neutralizes ligand-induced EGFR phosphorylation and downstream signaling, induces EGFR internalization and degradation, and mediates antibody-dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells. Necitumumab enhances antitumour activity in combination with Gemcitabine (HY-17026) and Cisplatin (HY-17394) in murine non-small-cell lung cancer xenograft models. Necitumumab can be used in research on cancers such as non-small cell lung cancer and colorectal cancer .
|
-
-
- HY-P99364
-
|
Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1
|
VEGFR
Apoptosis
p38 MAPK
Akt
|
Endocrinology
Cancer
|
|
Icrucumab (Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1) is an IgG1 antibody inhibitor targeting VEGFR-1/FLT1 with anti-tumor activity. By blocking ligand-dependent phosphorylation and downstream signal transduction, Icrucumab reduces the activities of MAPK and Akt in breast cancer xenograft models, inhibits the proliferation and invasion of VEGFR-1-positive tumor cells, and reverses the conversion of M1 macrophages to the pro-tumor M2-like phenotype. Icrucumab also inhibits tumor cell proliferation, promotes apoptosis, and effectively suppresses tumor growth through direct targeting of tumors and host support mechanisms. In addition, Icrucumab exhibits a synergistic effect when combined with chemotherapeutic agents, and it is used in research related to various cancers including advanced solid malignancies, thyroid cancer, melanoma, and lung cancer .
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-
-
- HY-N0841
-
|
Dihydrobrusatol; NSC310616
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Parasite
NF-κB
p38 MAPK
Phosphatase
Apoptosis
|
Infection
Cancer
|
|
Bruceine A (Dihydrobrusatol) is a natural quassinoid. Bruceine A is an inhibitor of parasites, NF-κB, and PFKFB4 (Kd: 44 nM). Bruceine A is an activator of P38α MAPK. Bruceine A has antiparasitic activity. Bruceine A has antitumor activity and inhibits cancer cell migration. Bruceine A blocks the cell cycle and induces apoptosis. Bruceine A can be used in parasites, pancreatic cancer, and breast cancer research .
|
-
-
- HY-N3980
-
Guaiol
1 Publications Verification
Champacol; Guaiac alcohol
|
Autophagy
RAD51
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
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-
-
- HY-P99943
-
|
KN-046
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PD-1/PD-L1
CTLA-4
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Cancer
|
|
Erfonrilimab (KN-046) is a monoclonal antibody targeting PD-L1/CTLA-4. Erfonrilimab blocks the PD-L1 and CTLA-4 pathways, thereby regulating T cell function. Erfonrilimab enhances the secretion of IL-2 in superantigen-stimulated peripheral blood mononuclear cells. Erfonrilimab inhibits tumor growth in xenograft and double gene knock-in mouse models. Erfonrilimab can be used in research related to a variety of advanced solid tumors, including non-small cell lung cancer and nasopharyngeal carcinoma.
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-
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- HY-P991669
-
|
AML-01
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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. .
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-
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- HY-132941
-
|
|
PROTACs
Epigenetic Reader Domain
c-Myc
Apoptosis
|
Cancer
|
|
CFT-2718 is a selective CRBN-dependent BRD4 PROTAC degrader. CFT-2718 mediates rapid, selective BRD4 degradation, reduces total and phosphorylated Ser2 RPB1 levels, and reduces MYC protein levels. CFT-2718 can inhibit cancer cells proliferation and induce apoptosis. CFT-2718 reduces growth of lung cancer and pancreatic patient-derived xenograft models. CFT-2718 can be used for the research of cancer, such as small-cell lung cancer and pancreatic cancer .
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-
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- HY-12929
-
|
SU093
|
Pim
Apoptosis
|
Cancer
|
|
NSC756093 (SU093) is a GBP1:PIM1 interaction inhibitor. NSC756093 binds to GBP1-PIM1 with a Kd of 38 nM. NSC756093 suppresses proliferation, reduces migration, induces G1 phase cell-cycle arrest, and increases apoptotic cell death in ovarian cancer cells. NSC756093 reduces cellular proteasomal activity, induces accumulation of ubiquitinated proteins, and restrains tumor progression and lung metastasis in murine ovarian cancer xenograft models. NSC756093 increases sensitivity of prostate cancer cells to Docetaxel (HY-B0011) and sensitizes GBP1-overexpressing ovarian cancer cells to Paclitaxel (HY-B0015). NSC756093 can be used for the research of prostate cancer and ovarian cancer .
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-
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- HY-175839
-
|
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PROTACs
EGFR
ATP Synthase
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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)) .
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-
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- HY-170428
-
|
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Molecular Glues
Ras
Ligands for E3 Ligase
|
Cancer
|
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IPS-06061 is an orally active molecular glue forming a ternary complex of CRBN-KRAS G12D-IPS06061, degrading KRAS G12D with a DC50 value lower than 500 nM. IPS-06061 shows a strong anti-tumor efficacy .
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-
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- HY-117366
-
|
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PKC
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Cancer
|
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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 .
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-
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- HY-174346
-
|
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E1/E2/E3 Enzyme
Apoptosis
DNA/RNA Synthesis
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Cancer
|
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Skp2-IN-4 is an Skp2 inhibitor with a IC50 of 0.38 μM for Skp2-Cks1 binding. Skp2-IN-4 improves anti-tumor activity, inhibits the proliferation and induces S phase arrest by targeting Skp2. Skp2-IN-4 significantly enhances Cisplatin (HY-17394) chemosensitivity by suppressing the tumor cell stemness in NCl-H1299 xenograft mice model, promising for lung cancer and esophageal cancer research .
|
-
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- 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)) .
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-
-
- HY-170824
-
|
|
PROTACs
SWI/SNF Complex
Epigenetic Reader Domain
|
Cancer
|
|
SMD-3236 is a SMARCA2 PROTAC degrader with a DC50 of 0.5 nM, a Dmax of 98%, and an IC50 of 42.2 nM against human SMARCA2. SMD-3236 induces proteasome- and ubiquitin-like modification-dependent degradation of SMARCA2 protein by binding to SMARCA2 and VHL-1. SMD-3236 inhibits the growth of SMARCA4-deficient cancer cells. SMD-3236 induces significant and persistent depletion of SMARCA2 in tumor tissues. SMD-3236 suppresses tumor growth in SMARCA4-deficient human cancer xenograft models. SMD-3236 can be used in research related to SMARCA4-deficient cancers such as melanoma, non-small cell lung cancer, and acute myeloid leukemia .
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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) .
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-
-
- HY-165245
-
|
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Transmembrane Glycoprotein
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Cancer
|
|
SBI-183 is an orally active inhibitor of QSOX1 (Kd: 20 μM). SBI-183 suppresses the proliferative and invasive phenotype of renal cancer cell lines, including triple negative breast cancer cell line, lung adenocarcinoma cell line and pancreatic ductal adenocarcinoma. SBI-183 inhibits tumor growth in two human xenograft mouse models of renal cell carcinoma in vivo .
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-
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- HY-175729
-
|
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CDK
|
Cancer
|
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Cyclin A/B RxL-IN-1 is a inhibitor targeting the Cyclin A/B RxL interaction at the hydrophobic patch (HP). Cyclin A/B RxL-IN-1 inhibits Cyclin A with an IC50 of 0.12 μM. Cyclin A/B RxL-IN-1 demonstrates antitumor efficacy in mouse cell line-derived xenograft (CDX) models. CDK-IN-19 can be used for the study of E2F-driven cancers such as small-cell lung cancer (SCLC) .
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-
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- HY-148278
-
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SOS1
Ras
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Cancer
|
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BI-0474 is a potent KRAS G12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models .
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-
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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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-
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- HY-P990947
-
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AZD9592 Antibody
|
ADC Antibody
EGFR
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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) .
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-
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- HY-178238
-
|
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ADC Payload
Topoisomerase
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Cancer
|
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LD2-3 is a cytotoxic compound derived from Exatecan (HY-13631), designed to be conjugated with anti-FGFR2b or anti-CEA antibodies to form intact antibody-drug conjugate (ADC) molecules. LD2-3 exhibits a remarkable bystander killing effect: it not only effectively kills FGFR2b-positive tumor cells, but also eliminates surrounding FGFR2b-negative cells in co-culture and mixed tumor xenograft models, thereby inducing complete tumor regression. LD2-3 can be used for anti-tumor research in relevant fields such as gastric cancer and lung cancer .
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-
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- HY-P990953
-
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Gen1047
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CD3
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Cancer
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Zubotamig (Gen1047) is an CD3E/VTCN1-targeting Ig(G1 -κ_G1 -λ2) type chimeric human antibody. The recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001). Zubotamig induces T-cell mediated cytotoxicity of B7H4-positive tumor cells, triggers T-cell activation, and induces cytokine release from T cells in the presence of B7H4-expressing tumor cells. Zubotamig demonstrates antitumor activity in mouse patient-derived xenograft (PDX) models. Zubotamig can be used for the research of solid cancers (including breast, ovarian and lung cancer) .
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- HY-177332
-
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TAM Receptor
SARS-CoV
Akt
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Infection
Cancer
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SLC-391 is an orally active AXL kinase inhibitor with an IC50 of 9.6 nM against AXL kinase. SLC-391 inhibits Gas6-induced AXL-dependent phosphorylation of Akt. SLC-391 inhibits SARS-CoV-2 infection, entry and replication in cells. SLC-391 suppresses cancer cell proliferation. SLC-391 inhibits tumor growth in mouse solid tumor xenograft models. SLC-391 can be used for the research of COVID-19, influenza virus infection, triple-negative breast cancer, chronic myeloid leukemia and non-small cell lung cancer .
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-
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- HY-178367
-
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Phosphatase
Apoptosis
Caspase
PARP
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Cancer
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PFKFB4-IN-1 is a potent and selective ATP-competitive PFKFB4 inhibitor (IC50 = 4.50 μM) that reduces intracellular PFKFB4 protein levels. PFKFB4-IN-1 exhibits >12-fold selectivity over PFKFB1/4 and PFKFB3/4. PFKFB4-IN-1 inhibits cancer cell proliferation, induces apoptosis, and inhibits cell migration. PFKFB4-IN-1 inhibits tumor growth in the MDA-MB-231 xenograft mouse model. PFKFB4-IN-1 can be used for breast, lung and liver cancer research .
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- HY-P10759
-
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Peptide-Drug Conjugates (PDCs)
Aminopeptidase
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Cancer
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DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
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-
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- HY-144898
-
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Microtubule/Tubulin
Apoptosis
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Cancer
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SB-216 is an BBB-penetrable tubulin polymerization inhibitor. SB-216 can inhibit the proliferation and migration, and induce apoptosis and cell cycle arrest of tumor cells. SB-216 has good in vivo metabolic stability and low toxicity, but its oral bioavailability is limited. SB-216 has antitumor activity and can be used in the research of tumors such as melanoma .
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- HY-146223
-
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Ras
p38 MAPK
PI3K
Apoptosis
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Cancer
|
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AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRASG12C inhibitor with an IC50 of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. AZD4625 can be used for the study of KRASG12C mutant non-small cell lung cancer .
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- HY-170978
-
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PROTACs
CDK
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Cancer
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PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC degrader for CDK9 with DC50 of 1.09 nM. PROTAC CDK9 degrader-11 exhibits cytotoxicity in multi small cell lung cancer cell with IC50 of nanomolar levels. PROTAC CDK9 degrader-11 arrests cell cycle at G0/G1 phase, inhibits the cell invasion in DMS114 and DMS53 cell. PROTAC CDK9 degrader-11 exhibits antitumor efficacy in NCI-H446 xenograft mouse models .(Pink: ligand for target protein CDK9 ligand 3 (HY-170979); Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56 (HY-W247437))
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- HY-P10988
-
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Apoptosis
MDM-2/p53
Integrin
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Cancer
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LVTX-8 is a peptide toxin, exacted from Lycosa vittata. LVTX-8 has potent anticancer and and anti-metastasis activities towards lung cancer with strong cytotoxicity. LVTX-8 significantly induces apoptosis and inhibits the proliferation, invasion and migration of lung cancer cells through P53 hypoxia pathways and integrin signaling. LVTX-8 significantly inhibits the tumor growth and metastasis in A549/H460 xenograft mice model .
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-
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- HY-174315
-
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PROTACs
Anaplastic lymphoma kinase (ALK)
Akt
ERK
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Cancer
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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-103043
-
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Others
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Cancer
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Pz 285 is an anti-cancer agent. Pz 285 shows significant inhibitory effect on the viability of MDA-MB-231 breast cancer cells, with an IC50 of 15.0 μM. Pz 285 exhibits remarkable antitumor effects in the mouse tumor xenograft model constructed with highly lung-metastatic MDA-MB-231 LM24 Her2+ breast cancer cells. Pz 285 can be used for the study of breast cancer, especially metastatic breast cancer .
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- HY-178008
-
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Bcl-2 Family
Caspase
Apoptosis
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Cancer
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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) .
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- HY-N2199
-
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Apoptosis
Autophagy
PI3K
JNK
mTOR
p38 MAPK
CDK
MMP
TGF-beta/Smad
STAT
β-catenin
Reactive Oxygen Species (ROS)
Bcl-2 Family
Caspase
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Inflammation/Immunology
Cancer
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Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits phosphorylation of PI3K, Akt, mTOR, JNK, and p38 MAPK; modulates expression of Cyclin D1, CDK4, Bcl-2, Bax, cleaved caspases 3/9, MMP-9, TGF-β, STAT3, and β-catenin. Sotetsuflavone induces G0/G1 cell cycle arrest, apoptosis, autophagy, and intracellular ROS elevation, inhibits cancer cell proliferation. Sotetsuflavone inhibits tumor growth in mouse tumor xenograft models. Sotetsuflavone can be used for the research of non-small cell lung cancer and Crohn’s disease .
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- HY-178391
-
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ROS Kinase
p38 MAPK
ERK
Apoptosis
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Cancer
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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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-
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- HY-175318S
-
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MDM-2/p53
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Cancer
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p53 Activator 15 is an orally active p53 Y220C activator. p53 Activator 15 enhances the DNA binding of p53 Y220C (SC50 = 0.58 nM) and significantly inhibits NUGC-3 cell proliferation. p53 Activator 15 effectively inhibits tumor growth in NUGC-3 xenograft mouse and rat models. p53 Activator 15 can be used to study gastric cancer .
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- HY-175206
-
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P-glycoprotein
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Cancer
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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-W110138
-
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DNA/RNA Synthesis
Cytochrome P450
ROCK
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Cancer
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Chloroxoquinoline is an anticancer agent. Chloroxoquinoline damages the DNA templates of cancer cells, inducing DNA breaks and cell death, and inhibits cell invasion via down-regulating Rho/Rho kinase signaling pathway. Chloroxoquinoline enhances the radiation sensitivity of Lewis lung cancer cells and xenograft tumors in tumor-bearing mouse models but decreases efficacy after long term exposure in rat models by auto-induction effects on CYP1A and CYP3A. Chloroxoquinoline has a broad-spectrum anticancer activity, such as non-small-cell lung carcinoma (NSCLC), breast cancer and gastric cancer .
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- HY-144361
-
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Apoptosis
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Cancer
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Antitumor agent-44 (Compound 5n) disrupts the mitochondrial homeostasis, induces cell cycle arrest and apoptosis in human adenocarcinoma cells. Antitumor agent-44 (Compound 5n) possesses good anti-tumor activity in a lung-cancer-cell xenograft mice model .
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- HY-114253
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EGFR
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Cancer
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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-168300
-
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Reactive Oxygen Species (ROS)
Apoptosis
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Inflammation/Immunology
Cancer
|
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Antiangiogenic agent 7 (Compound 1) can induce cell apoptosis, increase Reactive Oxygen Species, and inhibit the intracellular enzyme thioredoxin reductase. Antiangiogenic agent 7 has anti-cancer activity, with an IC50 of 0.08-3.5 μM against cervical cancer cells HeLa, prostate cancer cells PC-3, and non-small cell lung cancer A549. Antiangiogenic agent 7 inhibits tumor growth in mouse xenograft models .
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- HY-106154
-
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Peptide-Drug Conjugates (PDCs)
Aminopeptidase
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Cancer
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DTS-201 (CPI-0004) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
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- HY-120638
-
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Topoisomerase
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Cancer
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BMS-250749 is a topoisomerase I (Top I) inhibitor of the fluoroglycosyl-3,9-difluoroindolecarbazole class. BMS-250749 exhibits potent cytotoxicity and selectivity, and shows curative antitumor activity against Lewis lung cancer. BMS-250749 exhibits broad-spectrum antitumor activity superior to CPT-11 in certain preclinical xenograft models. .
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-
-
- HY-175820
-
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VEGFR
ERK
Apoptosis
EGFR
|
Cancer
|
|
AGW-11 is a potent dual inhibitor of EGFR (IC50 = 556 nM) and VEGFR2 (IC50 = 289.7 nM). AGW-11 induces apoptosis and suppresses phosphorylation of EGFR, VEGFR2, and ERK1/2 in HUVECs. AGW-11 effectively inhibits cancer cell growth, reduces HUVEC proliferation, tube formation, and invasion, thereby blocking angiogenesis. AGW-11 significantly suppresses tumor growth and decreases lung metastasis in a 4T1 xenograft mouse model. AGW-11 can be used for the study of breast cancer .
|
-
-
- HY-149695
-
|
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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 .
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-
-
- HY-170968
-
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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 .
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-
-
- HY-123237
-
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c-Met/HGFR
FLT3
Trk Receptor
Apoptosis
Autophagy
|
Cancer
|
|
KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice .
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-
-
- 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 .
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-
- HY-178451
-
|
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Apoptosis
|
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-172256
-
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PI4K
|
Cancer
|
|
PI4KIII beta inhibitor 5 is a PI4KIIIβ inhibitor with an IC50 of 19 nM. PI4KIII beta inhibitor 5 can induce cancer cell apoptosis (Apoptosis), cell cycle arrest at the G2/M phase, and autophagy (Autophagy) by inhibiting the PI3K/AKT pathway. PI4KIII beta inhibitor 5 has also demonstrated significant antitumor activity in the H446 xenograft model of small cell lung cancer. PI4KIII beta inhibitor 5 can be used for research in the field of cancer therapy .
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-
- HY-12965B
-
|
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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) .
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-
- HY-176942
-
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ROS1-IN-3
|
ROS Kinase
Trk Receptor
|
Cancer
|
|
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) .
|
-
- HY-150774
-
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HDAC
HSP
Apoptosis
|
Cancer
|
|
HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor of HDAC6 and Hsp90, with IC50s of 105.7 and 61 nM, respectively. HDAC6/HSP90-IN-2 can be used for the research of cancer .
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-
- HY-171509
-
|
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Drug-Linker Conjugates for ADC
Apoptosis
|
Cancer
|
|
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) .
|
-
- HY-172795
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-158 (compound 12e) is an orally active EGFR inhibitor with an IC50 of 0.22 nM for EGFR(Del19/T790M). EGFR-IN-158 inhibits phosphorylation and downstream signaling by binding to EGFR, thereby inhibiting the proliferation of tumor cell lines and promoting apoptosis .
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-
- HY-N3980R
-
|
Champacol (Standard); Guaiac alcohol (Standard)
|
Reference Standards
Autophagy
RAD51
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Guaiol (Standard) is the analytical standard of Guaiol. This product is intended for research and analytical applications. Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
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-
- HY-181650
-
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mTOR
Akt
Ribosomal S6 Kinase (RSK)
Apoptosis
Autophagy
PI3K
|
Cancer
|
|
T133 is an orally active ATP-competitive mTOR inhibitor with an IC50 of 0.34 nM and a Ki of 0.17 nM. T133 suppresses phosphorylation of AKT, S6K1, and 4EBP1. T133 inhibits cancer cell proliferation and migration, induces apoptosis, cell cycle arrest, and autophagy. T133 exhibits dose-dependent antitumor efficacy in xenograft mouse models. T133 can be used for the research of cancer, such as gastric cancer and lung cancer .
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-
- HY-180430
-
|
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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-181517
-
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Bacterial
|
Infection
Cancer
|
|
Antitumor agent-212 is a α-exo-methylene-selenolactone derivative with prominent selective antitumor activity. Antitumor agent-212 exhibits an MIC value of 128 μg/mL against Gram-positive bacteria. Antitumor agent-212 exhibits significant antitumor effects in the U87 human glioma xenograft model. Antitumor agent-212 can be used for the study of glioma, breast cancer and non-small cell lung cancer, and antibacterial study .
|
-
- HY-P992158
-
|
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CD47
|
Cancer
|
|
VBI-009 is a CD47 and B7-H3 (CD276) bispecific antibody. VBI-009 blocks CD47-SIRPα 'don't eat me' signals and restricts activity to CD47 +/B7-H3 + cells. VBI-009 induces antibody-dependent cellular phagocytosis (ADCP) and antibody-dependent cellular cytotoxicity (ADCC) in CD47 +/B7-H3 + tumor cells. VBI-009 inhibits tumor growth in CD47+/B7-H3+ lung cancer xenograft models. VBI-009 can be used for the research of lung cancer .
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-
- HY-181550A
-
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Cytochrome P450
P-glycoprotein
|
Cancer
|
|
CYP1B1-IN-14 TFA is a metabolically stable hCYP1B1 competitive inhibitor with an IC50 of 1.32 nM and a Ki of 0.72 μM. CYP1B1-IN-14 TFA reverses the resistance of cancer cells to Paclitaxel (HY-B0015). CYP1B1-IN-14 TFA acts synergistically with Paclitaxel (HY-B0015) to inhibit tumor growth in xenograft models without obvious toxicity. CYP1B1-IN-14 TFA can be used for the research of cancers such as paclitaxel-resistant lung cancer .
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-
- HY-182378
-
|
|
|
Cancer
|
|
Vps34-IN-5 is an orally active VPS34 inhibitor, 98% target inhibition, and an IC50 categorized as B. Vps34-IN-5 induces additive or synergistic anti-proliferative activity with EGFR inhibitors in cancer cells. Vps34-IN-5 is administered orally alone or with Erlotinib (HY-50896) in mouse xenograft models. Vps34-IN-5 can be used for the research of non-small cell lung cancer .
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-
- HY-180200
-
|
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Ras
ERK
|
Cancer
|
|
RNK08954 is an orally active KRASG12D inhibitor with a Kd of 0.0395 nM. RNK08954 selectively binds the inactive GDP-bound KRASG12D form, suppresses downstream KRAS-mediated signaling pathways p-ERK1/2 experssion. RNK08954 inhibits KRASG12D-mutant cell proliferation, induces G0-G1 cell cycle arrest, and inhibits tumor growth in mouse xenograft models. RNK08954 can be used for the research of non-small cell lung cancer, pancreatic ductal adenocarcinoma .
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-
- HY-181943
-
|
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Acyltransferase
|
Cancer
|
|
SPT-IN-2 is an orally active serine palmitoyltransferase (SPT) inhibitor (with an IC50 of 0.71 nM against human SPT2). SPT-IN-2 inhibits ceramide synthesis, suppresses cancer cell growth, and exhibits in vivo anti-tumor activity, favorable metabolic stability and cell membrane permeability in xenograft mouse models. SPT-IN-2 blocks the de novo sphingolipid synthesis pathway, significantly reducing intracellular ceramide levels and the levels of 3-ketodihydrosphingosine (3-KDS), the immediate downstream product of SPT. SPT-IN-2 can be used in research related to lung adenocarcinoma, acute promyelocytic leukemia and breast cancer .
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-
- HY-181420A
-
|
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Ras
Phosphatase
ERK
Apoptosis
|
Cancer
|
|
BBO-11818 is an orally active, highly selective (relative to NRAS and HRAS), non-covalent pan-KRAS inhibitor (IC50=28-120 nM). BBO-11818 specifically binds to the Switch-II/Helix 3 pocket, disrupts the KRAS:RAF1 interaction by inducing conformational changes, and blocks the MAPK signaling pathway. BBO-11818 exhibits significant anti-tumor activity, which not only inhibits cell proliferation and induces apoptosis, but also drives tumor regression in xenograft models. BBO-11818 produces synergistic effects when combined with Cetuximab (HY-P9905), anti-PD-1 antibody or PI3Kα inhibitor. BBO-11818 is used in the research of KRAS mutation-related malignancies such as pancreatic cancer, non-small cell lung cancer and colorectal cancer .
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-
- HY-116636
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
KRCA-0377 is an orally active ALK inhibitor with an IC50 of 0.001 μM. KRCA-0377 also inhibits mutant ALK enzyme with IC50 values ≤0.01 μM. KRCA-0377 shows cytotoxicity against cancer cells and inhibits tumor growth in xenograft mice models. KRCA-0377 can be used for the research of ALK-positive non-small-cell lung cancer .
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-
- HY-183007
-
|
|
PROTACs
SWI/SNF Complex
|
Cancer
|
|
LJM133 is a SMARCA2/PBRM1/SMARCA4 PROTAC degrader with DC50 values of 3.5 nM, 7 nM, and 6.4 nM. LJM133 induces ternary complex formation with VHL E3 ligase to drive proteasome-mediated degradation of target proteins. LJM133 suppresses cell proliferation and exhibits significant antitumor efficacy in a SMARCA4 mutant cancer xenograft model. LJM133 can be used for the research of cancer, such as SMARCA4 mutant non-small cell lung cancer . (Pink: SMARCA2/PBRM1/SMARCA4 ligand (HY-182987); E3 ubiquitin ligase ligand-linker conjugate (HY-183619)).
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-
- HY-P992338
-
|
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Mesothelin
Constitutive Androstane Receptor
|
Inflammation/Immunology
Cancer
|
|
CT-1119 is an autologous human anti-Mesothelin chimeric antigen receptor macrophage (CAR-M). CT-1119 mediates CAR-dependent, antigen-dependent functional activities. CT-1119 acts as a phagocytosis inducer, tumor cell killer, pro-inflammatory cytokine inducer, and M1 macrophage polarizer. CT-1119 exhibits stronger resistance to M2 repolarization and reduces tumor burden in a mouse lung cancer xenograft model. CT-1119 can be used for the research of mesothelin-expressing solid tumors .
|
-
- HY-186086
-
|
|
Ras
|
Cancer
|
|
RM-041 is a selective, orally active KRAS G13C (ON) inhibitor that forms a covalent complex with KRAS G13C (ON) and Cyclophilin A. RM-041 blocks the binding of RAS effector proteins via steric hindrance, and then covalently binds to Cys-13 to form an irreversible inhibitory complex, thereby inhibiting the proliferation of KRAS G13C mutant cancer cells. RM-041 induces regression of KRAS G13C tumors in cellular and xenograft tumor models. RM-041 exerts a synergistic effect when combined with upstream node inhibitors (such as SHP2 inhibitors). RM-041 can be used for the research of non-small cell lung cancer .
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-
- HY-165503
-
|
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Wnt
β-catenin
|
Cancer
|
|
AZ1366 is an orally active tankyrase inhibitor. AZ1366 stabilizes Axin2, reduces NuMA levels, disrupts the interaction between tankyrase and NuMA, induces G2/M phase arrest, inhibits the Wnt pathway, and downregulates the expression of β-catenin-dependent genes. AZ1366 inhibits tumor growth in colorectal cancer xenograft models. AZ1366 synergistically inhibits the proliferation of non-small cell lung cancer cells, improves tumor control and significantly prolongs survival in orthotopic non-small cell lung cancer mouse models. AZ1366 is applicable to research related to colorectal cancer and non-small cell lung cancer .
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-
- HY-181777
-
|
|
EGFR
|
Cancer
|
|
Mal-Pip-ValCit-PAB-AZ7550 is a prodrug of EGFR inhibitor. Mal-Pip-ValCit-PAB-AZ7550 selectively binds covalently to albumin via its maleimide moiety. Mal-Pip-ValCit-PAB-AZ7550 exhibits potent in vivo anticancer activity in non-small cell lung cancer xenograft models. Mal-Pip-ValCit-PAB-AZ7550 can be used in research related to non-small cell lung cancer .
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-
- HY-153503
-
|
|
Anaplastic lymphoma kinase (ALK)
Insulin Receptor
|
Cancer
|
|
ALK-IN-24 is an orally active ALK inhibitor with an IC50 value of 1.7 nM. ALK-IN-24 also inhibits insulin receptor kinase with an IC50 value of 6 nM. ALK-IN-24 suppresses the proliferation of lung adenocarcinoma cells. ALK-IN-24 inhibits ALK-driven tumor growth in xenograft mouse models. ALK-IN-24 can be used in research related to non-small cell lung cancer .
|
-
- HY-180551
-
|
|
PROTACs
RET
Trk Receptor
|
Endocrinology
Cancer
|
|
ZW-6-052 (compound 20), the derivative of ZW-18-116 (HY-180550), is a dual-target PROTAC degrader for the oncoproteins TRKA and RET. ZW-6-052 induces degradation of TMP3-TRKA in KM12 mouse xenograft models. ZW-6-052 can be used for RET or TRKA-derived cancer research, such as thyroid, lung, and colon cancers .
|
-
- HY-P991999
-
|
|
FGFR
IFNAR
Interleukin Related
|
Cancer
|
|
OM-RCA-01 is an anti-FGFR1 monoclonal antibody with a Kd of 1.59 nM for human FGFR1. OM-RCA-01 inhibits the phosphorylation of FGFR1, blocks FGF-mediated signaling pathways, and suppresses the proliferation of downstream tumor cells. OM-RCA-01 delays tumor growth in lung cancer and renal cancer xenograft models expressing FGFR1. When combined with Nivolumab, OM-RCA-01 enhances the release of IFN-γ and IL-2. OM-RCA-01 is applicable for the research of lung cancer and renal cell carcinoma .
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-
- 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 .
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-
- 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-P992341
-
|
|
MMP
|
Cancer
|
|
D8P1C1 is a high-affinity ADAM17 inhibitor (with a Kd of 180 pM targeting ADAM17-ECD) that reduces the shedding and phosphorylation of EGFR ligands. D8P1C1 inhibits cancer cell proliferation in vitro and tumor growth in xenograft models. 89Zr-DFO-D8P1C1 radioimmunological PET imaging shows its substantial accumulation in ovarian tumor xenografts, serving as a platform for generating bispecific T-cell engager derivatives. D8P1C1 can be applied to research on related diseases including triple-negative breast cancer, various types of ovarian cancer, lung adenocarcinoma, glioma, and colon cancer .
|
-
- HY-182764A
-
|
|
CDK
|
Cancer
|
|
CDK11-IN-1 hydrochloride is a potent, highly selective, and orally active CDK11 inhibitor with an IC50 of 4 nM, showing 32.5-fold and 2700-fold selectivity over CDK7 and CDK9, respectively. CDK11-IN-1 hydrochloride binds competitively to the ATP-binding pocket of CDK11 and forms a hydrogen bond with the hinge region residue Val163. It inhibits tumor cell proliferation and exhibits antitumor activity in lung cancer xenograft models. CDK11-IN-1 hydrochloride can be used for studies on the pathophysiology of CDK11-mediated tumors, as well as research on malignant tumors such as lung cancer .
|
-
- HY-183116
-
|
|
Molecular Glues
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
TRI-611 is a brain-penetrant, orally active molecular glue degrader targeting ALK. TRI-611 engages ALK via a distal degron, forms a ternary complex with CRBN, triggers ALK polyubiquitination and degradation, including TKI-resistant ALK fusion proteins. TRI-611 inhibits ALK downstream signaling pathways, induces anti-proliferative effects in ALK-positive cancer cells. TRI-611 induces regression of ALK-positive non-small cell lung cancer tumors in preclinical xenograft models. TRI-611 can be used for the research of ALK-positive non-small cell lung cancer, including TKI-refractory tumors and central nervous system metastases .
|
-
- HY-P992146
-
|
MYTX-011 Antibody; Q-397
|
ADC Antibody
c-Met/HGFR
|
Cancer
|
|
Zevontabart (MYTX-011 Antibody; Q-397) is a pH-dependent anti-c-MET antibody. Zevontabart regulates the trafficking process of c-MET to reduce receptor recycling, and enhances its own endocytosis and accumulation in c-MET-expressing cells. Zevontabart induces cytotoxicity in solid tumor cells and exerts anti-tumor activity in a non-small cell lung cancer xenograft mouse model. Zevontabart can be used to synthesize ADC, such as: MYTX-011. Zevontabart can be used in studies related to non-small cell lung cancer, with its corresponding isotype control being Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-183568
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A-IN-26 is an orally active MAT2A inhibitor with a human IC50 of 17.53 nM. MAT2A-IN-26 inhibits the enzymatic activity of MAT2A, thereby reducing the levels of S-adenosylmethionine (SAM) and symmetric dimethylarginine (sDMA). MAT2A-IN-26 inhibits the proliferation of MTAP-deficient cancer cells and induces anti-tumor efficacy in xenograft models. MAT2A-IN-26 can be used in non-small cell lung cancer research .
|
-
- HY-183120
-
|
|
FAK
EGFR
Apoptosis
|
Cancer
|
|
EGFR T790M/FAK-IN-2 is an orally active dual FAK and EGFR T790M kinase inhibitor, with an IC50 of 1.03 nM against FAK and an IC50 of 3.89 nM against EGFR T790M. EGFR T790M/FAK-IN-2 exerts antiproliferative effects in drug-resistant cancer cells overexpressing FAK, inducing apoptosis and cell cycle arrest. EGFR T790M/FAK-IN-2 exhibits antitumor activity in a pancreatic cancer xenograft mouse model. EGFR T790M/FAK-IN-2 can be used for the research of pancreatic cancer, breast cancer and non-small cell lung cancer .
|
-
- HY-182382
-
|
|
Apoptosis
MDM-2/p53
Caspase
|
Cancer
|
|
Anticancer agent 311 is an apoptosis inducer and p53 modulator. Anticancer agent 311 increases p53 levels, activates cleaved caspase-3, reduces p-Cdc25C levels, and disrupts p-p44/42 MAPK phosphorylation. Anticancer agent 311 induces G2/M phase arrest, inhibits cancer cell viability in a concentration- and time-dependent manner, and exhibits low toxicity to non-cancer cells. Anticancer agent 311 prevents tumor growth and angiogenesis in mouse xenograft models without detectable toxicity. Anticancer agent 311 can be used for the research of lung cancer .
|
-
- HY-181838
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CIRc-014 is an orally active Cyclin A/B inhibitor with a Cyclin A IC50 of 0.05 μM, Cyclin A Kd of 2.7 nM, Cyclin B IC50 of less than 0.02 μM and Cyclin B Kd of 1.0 nM. CIRc-014 activates the spindle assembly checkpoint and promotes the formation of a complex between Cyclin B and CDK2 by blocking the RxL interaction of Cyclin A/B. CIRc-014 can induce replication stress, DNA damage, mitotic arrest and apoptosis in tumor cells. CIRc-014 showed tumor growth inhibition and regression in NCI-H69 and NCI-H446 small cell lung cancer xenograft models. CIRc-014 can be used for the research of small-cell lung cancer .
|
-
- HY-181716
-
|
|
Ras
Apoptosis
|
Cancer
|
|
KRAS G12C-IN-74 is an orally active, selective KRAS G12C inhibitor with a target IC50 of 43.18 nM. KRAS G12C-IN-74 induces G0/G1 cell cycle arrest and apoptosis in KRAS G12C-mutant cancer cells. KRAS G12C-IN-74 is applicable for the research of KRAS G12C-mutant pancreatic cancer, colorectal cancer and lung cancer .
|
-
- HY-109061R
-
|
YH25448 (Standard); GNS-1480 (Standard)
|
Apoptosis
Akt
TRP Channel
EGFR
ERK
Reference Standards
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Lazertinib (Standard) is the analytical standard of Lazertinib (HY-109061). This product is intended for research and analytical applications. Lazertinib (YH25448) is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib can be used in the study of non-small cell lung cancer .
|
-
- HY-109061BR
-
|
YH25448 mesylate (Standard); GNS-1480 mesylate (Standard)
|
Reference Standards
|
Cancer
|
|
Lazertinib mesylate (Standard) is the analytical standard of Lazertinib (mesylate) (HY-109061B). This product is intended for research and analytical applications. Lazertinib (YH25448) mesylate is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib mesylate inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib mesylate can be used in the study of non-small cell lung cancer .
|
-
- HY-181954
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
ZW-49 is an orally active pan-EGFR inhibitor with IC50 values at 0.03-1.5 nM. ZW-49 inhibits all subgroups of EGFR mutations with selectivity over wild-type EGFR and other target families. ZW-49 blocks the ATP-binding pocket, occupies a conserved hydrophobic subpocket, avoids steric conflicts with PACC mutation P loops. ZW-49 inhibits cancer cells proliferation, induces G0/G1 phase cell-cycle arrest and apoptosis, and demonstrates anti-proliferative activity in xenograft mice models. ZW-49 can be used for the research of cancer, such as non-small cell lung cancer .
|
-
- HY-181687
-
|
|
HSP
CDK
|
Cancer
|
|
Hsp90-IN-46 is a Hsp90 inhibitor. Hsp90-IN-46 exhibits broad-spectrum antiproliferative activity against tumor cell lines. Hsp90-IN-46 inhibits breast cancer cell proliferation by reducing colony formation and downregulating the proliferation marker Ki-67. Hsp90-IN-46 inhibits Hsp90 and its ATPase activity, downregulates the downstream substrate oncoproteins HER2 and CDK4, and moderately induces the heat shock response. Hsp90-IN-46 shows significant antitumor activity in a mouse model of triple-negative breast cancer tumor xenografts. Hsp90-IN-46 can be used for research on various cancers including triple-negative breast cancer, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer .
|
-
- HY-183783
-
|
|
PROTACs
RET
STAT
ERK
Apoptosis
|
Endocrinology
Cancer
|
|
PROTAC RET Degrader 2 is a RET degrader with a target IC50 of 0.36 nM. PROTAC RET Degrader 2 is mainly composed of RET-IN-34 (HY-183729) and Thalidomide (HY-14658). PROTAC RET Degrader 2 mediates RET degradation via the ubiquitin-proteasome system. PROTAC RET Degrader 2 induces apoptosis, inhibits colony-forming ability, and exhibits antiproliferative activity in cancer cells. PROTAC RET Degrader 2 suppresses tumor growth in xenograft models. PROTAC RET Degrader 2 can be used in research related to medullary thyroid carcinoma, papillary thyroid carcinoma, and RET fusion-positive lung adenocarcinoma .
|
-
- HY-180818
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
ALK-IN-33 (Compound 8q) is an orally active ALK inhibitor with an IC50 of 1.61 nM. ALK-IN-33 exhibits significant selective killing effect on ALK-positive cancer cells. ALK-IN-33 induces cell cycle arrest and apoptosis, effectively weakening the migration, invasion and long-term survival ability of cancer cells. ALK-IN-33 can be used for research on non-small cell lung cancer
|
-
- HY-181889
-
|
|
Ras
|
Cancer
|
|
KRAS G12C-IN-75 is an orally active, blood-brain barrier penetrant KRAS G12C inhibitor with an IC50 of 0.53 nM. KRAS G12C-IN-75 attenuates active transport mediated by P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). KRAS G12C-IN-75 inhibits tumor growth, regulates the expression of downstream MAPK target genes DUSP6 and SPRY4, and exhibits dose-dependent KRAS G12C alkylation in KRAS G12C-positive xenograft models. KRAS G12C-IN-75 can be used for research related to non-small cell lung cancer .
|
-
- HY-183257
-
|
|
Autophagy
Beclin1
Reactive Oxygen Species (ROS)
p97
|
Cancer
|
|
ATI-1 is an autophagy initiation inhibitor. ATI-1 targets valosin-containing protein (VCP/p97, disrupts its interaction with UFL1, impairs UFMylation homeostasis associated with VCP, promotes polyubiquitination and degradation of Beclin1, and blocks the formation of early autophagosomes. ATI-1 induces synergistic death of autophagy-dependent malignant tumor cells under nutrient deprivation conditions, accompanied by decreased mitochondrial membrane potential, reduced ROS levels and lysosomal stress. ATI-1 exhibits anti-tumor efficacy in a pancreatic adenocarcinoma xenograft mouse model. ATI-1 can be used for the research of pancreatic adenocarcinoma and lung cancer .
|
-
- HY-181420
-
|
|
ERK
Apoptosis
Phosphatase
Ras
|
Cancer
|
|
(S,R,S)-BBO-11818 is an orally active, highly selective (relative to NRAS and HRAS), non-covalent pan-KRAS inhibitor (IC50=28-120 nM). (S,R,S)-BBO-11818 specifically binds to the Switch-II/Helix 3 pocket, disrupts the KRAS:RAF1 interaction by inducing conformational changes, and blocks the MAPK signaling pathway. (S,R,S)-BBO-11818 exhibits significant anti-tumor activity, which not only inhibits cell proliferation and induces apoptosis, but also drives tumor regression in xenograft models. (S,R,S)-BBO-11818 produces synergistic effects when combined with Cetuximab (HY-P9905), anti-PD-1 antibody or PI3Kα inhibitor. (S,R,S)-BBO-11818 is used in the research of KRAS mutation-related malignancies such as pancreatic cancer, non-small cell lung cancer and colorectal cancer .
|
-
- HY-181673
-
|
|
Microtubule/Tubulin
Apoptosis
Bcl-2 Family
Caspase
PARP
|
Cancer
|
|
ICD inducer-2 is a immunogenic cell death inducer. ICD inducer-2 binds to the colchicine binding site on tubulin to inhibit tubulin polymerization. ICD inducer-2 exhibits broad-spectrum antiproliferative activity across multiple cancer cell lines. ICD inducer-2 inhibits cells migration, causes G2/M phase and induces apoptosis. ICD inducer-2 promotes infiltration of CD4+ and CD8+ T cells into the tumor microenvironment. ICD inducer-2 downregulates antiapoptotic protein Bcl-2, upregulates proapoptotic proteins Bax and Bim-1, and increases cleaved caspase 3, cleaved caspase 9, and cleaved PARP levels. ICD inducer-2 overcomes paclitaxel resistance in xenograft models and achieves tumor growth inhibition. ICD inducer-2 can be used for the research of cancer, such as lung carcinoma .
|
-
- HY-P991967
-
|
MAB100 Antibody
|
EGFR
|
Cancer
|
|
AVID100 (MAB100) Antibody is a monoclonal antibody inhibitor targeting EGFR, which can be used to synthesize a novel antibody-drug conjugate (ADC) molecule AVID100. AVID100 Antibody is applicable to relevant research on breast cancer, head and neck cancer, and lung cancer .
|
-
- HY-P992163
-
|
|
Fc Receptor (FcR)
C-type Lectin-like Receptors (CTLRs)
|
Inflammation/Immunology
Cancer
|
|
23ME-01473 is an anti-ULBP6/2/5 antibody with enhanced Fc effector function, with a Kd of 0.053 nmol/L against hULBP6, 0.23 nmol/L against hULBP2, and 1.92 nmol/L against hULBP5. 23ME-01473 restores anti-tumor immunity by activating NKG2D and FcγRIIIa. 23ME-01473 exerts anti-cancer activity in non-small cell lung cancer PDX models. 23ME-01473 can be used for the research of non-small cell lung cancer .
|
-
- HY-185075
-
|
LY4050784
|
SWI/SNF Complex
|
Cancer
|
|
FHD-909 (LY4050784) is an orally active and selective SMARCA2 (BRM) ATPase inhibitor. FHD-909 potently inhibits purified BRM ATPase with an IC50 of 0.0025 μM and exhibits 35.69-fold selectivity for BRM over purified SMARCA4 (BRG1) ATPase. FHD-909 induces synthetic lethality, suppresses cell proliferation, modulates target gene expression, and achieves remarkable tumor growth inhibition and regression in SMARCA4-mutant cancer cells and xenograft models. FHD-909 can be used for the research of SMARCA4/BRG1-mutant cancers, advanced solid tumors, and BAF complex-related disorders .
|
-
- HY-183951
-
|
|
Histone Methyltransferase
|
Neurological Disease
Cancer
|
|
TNG456 is an orally active, CNS-penetrant, selective, MTA-cooperative PRMT5 inhibitor. TNG456 drives dose-dependent antitumor activity in mouse xenograft models. TNG456 can be used for the research of MTAP-null solid tumors, including gliomas, and CNS metastases .
|
-
- HY-182071
-
|
|
Drug Derivative
Apoptosis
CDK
ASK1
|
Cancer
|
|
MG16 is a prodrug of 10-Methoxycamptothecin (HY-N0446). MG16 downregulates CDK6 and upregulates ASK1. MG16 induces cell cycle arrest and Apoptosis. MG16 exhibits anticancer activity against Lewis lung carcinoma, small cell lung cancer, and non-small cell lung cancer .
|
-
- HY-183684
-
|
|
RET
VEGFR
PDGFR
Akt
ERK
|
Endocrinology
Cancer
|
|
RET-IN-33 is a moderately selective inhibitor of RET mutants. RET-IN-33 potently inhibits G810 mutants, with IC50 values of 4.43 nM (G810R), 3.28 nM (G810C) and 0.51 nM (G810S), respectively. RET-IN-33 also inhibits other RET mutants: V804M (IC50 0.73 nM), V804L (IC50 0.36 nM), Y806H (IC50 0.74 nM) and M918T (IC50 0.55 nM). RET-IN-33 also inhibits other kinases, with an IC50 of 1.50 nM against VEGFR2 and 1.60 nM against PDGFRα. RET-IN-33 blocks the autophosphorylation of RET mutants and the downstream SHC/AKT/ERK signaling pathway. RET-IN-33 selectively inhibits the proliferation of RET-driven cell models without affecting non-RET-dependent or normal cells. RET-IN-33 exhibits dose-dependent antitumor efficacy in RET-driven xenograft models. RET-IN-33 can be used for the research of medullary thyroid carcinoma, papillary thyroid carcinoma and non-small cell lung cancer .
|
-
- HY-169061
-
|
|
Histone Methyltransferase
Aminotransferases (Transaminases)
Lactate Dehydrogenase
|
Cancer
|
|
WQQ-345 is an orally active BCAT1 inhibitor with an IC50 values of 10.8 mM. WQQ-345 reduces cellular α-KG levels, upregulating H3K27me3 expression, decreasing glycolytic enzyme expression, and impairing glycolysis activity. WQQ-345 reduces colony formation, suppresses growth of BCAT1-high TKI-resistant lung cancer cells. WQQ-345 exerts in vitro and in vivo antitumor activity. WQQ-345 can be used for the research of TKI-resistant non-small cell lung cancer and TKI-resistant lung cancer .
|
-
- 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-175864
-
|
|
EGFR
Apoptosis
p38 MAPK
ERK
Akt
STAT
|
Inflammation/Immunology
Cancer
|
|
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 .
|
-
- 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-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-180850
-
|
|
PROTACs
Estrogen Receptor/ERR
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
ERB-2 is a selective ERβ PROTAC degrader. ERB-2 removes the inhibitory effect of ERβ on ROS, leading to the accumulation of ROS, mitochondrial damage, and ultimately triggering cell apoptosis (apoptosis). ERB-2 significantly inhibits tumor growth in the nude mouse model of NCI-H1975OR tumors. ERB-2 can be used for the study of non-small cell lung cancer .
|
-
- HY-173629
-
|
|
Ras
Apoptosis
|
Cancer
|
|
RMC-5127 is a small molecule inhibitor that binds to GTP-targeted KRAS G12V, with oral bioavailability and blood-brain barrier permeability. RMC-5127 inhibits the activities of the RAS and MAPK pathways, suppresses the proliferation of KRAS G12V-mutant cancer cells and induces their apoptosis. RMC-5127 can be used for the research of KRAS G12V-mutant non-small cell lung cancer, pancreatic ductal adenocarcinoma, colorectal cancer and intracranial KRAS G12V tumors .
|
-
- HY-183277
-
|
|
EGFR
p38 MAPK
Akt
Apoptosis
|
Cancer
|
|
EGFR-IN-209 (Compound 6g) is an orally active, selective EGFR Del19/T790M/C797S inhibitor with an IC50 of 0.056 μM. EGFR-IN-209 blocks the phosphorylation of EGFR and its downstream effector molecules (pMAPK, pAKT). EGFR-IN-209 induces Apoptosis. EGFR-IN-209 exhibits antitumor activity against Osimertinib (HY-15772)-resistant non-small cell lung cancer. EGFR-IN-209 can be used in research related to non-small cell lung cancer .
|
-
- HY-185561
-
|
RC88
|
Mesothelin
|
Cancer
|
|
Misitatug blivedotin (RC88) is an antibody-drug conjugate (ADC) targeting mesothelin (MSLN). Misitatug blivedotin binds to mesothelin and exhibits dose‐dependent antitumor activity. Misitatug blivedotin can be used for the research of ovarian cancer, non-squamous non-small-cell lung carcinoma, cervical cancer .
|
-
- HY-181629A
-
|
|
Aryl Hydrocarbon Receptor
Apoptosis
Caspase
Cytochrome P450
|
Cancer
|
|
ZSTK3744 hydrochloride is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 hydrochloride directly binds to AhR, upregulates the expression of AhR target genes including CYP1A1, CYP1B1 and TIPARP, and mediates cell growth inhibitory activity in triple-negative breast cancer cells. ZSTK3744 hydrochloride induces apoptosis in triple-negative breast cancer cells. ZSTK3744 hydrochloride exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer .
|
-
- HY-181964
-
|
|
|
Cancer
|
|
KRAS G12C-IN-77 is an orally active and selective KRAS G12C covalent dual-state inhibitor that binds with high affinity to both GDP-bound (inactive state) and GTP-bound (active state) KRAS G12C (IC50 = 133 nM). KRAS G12C-IN-77 rapidly inhibits ERK1/2 phosphorylation, induces the formation of covalent adducts with endogenous KRAS G12C, suppresses the expression of MAPK pathway genes, and inhibits the proliferation of KRAS G12C-mutant cells. KRAS G12C-IN-77 is applicable to research related to KRAS G12C-mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer .
|
-
- HY-181794
-
|
|
Apoptosis
|
Cancer
|
|
Z19024498 is a heat sensitizer. Z19024498 inhibits SAFB granule formation under heat stress conditions. Z19024498 enhances heat stress-induced Apoptosis. Z19024498 exerts anticancer activity against cervical cancer in synergy with heat stress .
|
-
- HY-164548
-
|
|
HSP
Apoptosis
PI3K
Akt
NF-κB
|
Inflammation/Immunology
Cancer
|
|
WK88-1 is an apoptosis inducer and Hsp90 client protein inhibitor with antiproliferative and immunomodulatory activities. WK88-1 inhibits signaling pathways such as PI3K/Akt and NF-κB, and induces mitochondrial dysfunction and cell cycle arrest. WK88-1 effectively suppresses cancer cell migration and invasion, and reverses various EGFR mutations and resistance to Gefitinib (HY-50895). WK88-1 also regulates the differentiation of monocytes and dendritic cells, blocks the expression of multiple chemokines, inhibits immune cell migration and M1 marker transcription, and restores impaired endocytic activity. WK88-1 has been used in studies of breast cancer, non-small cell lung cancer with various EGFR mutations or Met amplification, and atherosclerosis and other related diseases .
|
-
- HY-P99866
-
|
MEHD-7945A; RG 7597
|
EGFR
Akt
p38 MAPK
Apoptosis
|
Cancer
|
|
Duligotuzumab (MEHD-7945A; RG 7597) is a humanized IgG-κ monoclonal antibody targeting EGFR. Duligotuzumab blocks the binding of ligands to these two receptors, inhibits downstream HER/ErbB, AKT and MAPK signaling pathways, induces antibody-dependent cellular cytotoxicity, reduces the proliferation and migration abilities of cancer cells, promotes apoptosis, exerts radiosensitizing effects, and reverses EGFR resistance in cancer cells. Duligotuzumab can be used in tumor-related research .
|
-
- HY-183741
-
|
|
PI3K
Akt
|
Cancer
|
|
VVD-844 is an orally active covalent inhibitor of PI3Kα, which inhibits Pl3Kα/p110α interaction with an IC50 of 4 nM. VVD-844 covalently binds to Cys 242 in the RAS binding domain of p110α, blocking RAS-p110α interaction and inhibiting PI3Kα activity. VVD-844 inhibits PI3Kα signaling activation in HER2-overexpressing cells via a RAS-independent mechanism. VVD-844 suppresses tumor growth in mouse. VVD-844 can be used for the research of cancers .
|
-
- HY-182624
-
|
|
Na+/H+ Exchanger (NHE)
Wnt
Apoptosis
|
Cancer
|
|
FJ9 is a NHERF1/PDZ inhibitor with human NHERF1 PDZ1 IC50 1540 μM, NHERF1 PDZ2 IC50 160 μM, and Frizzled-7-Dishevelled PDZ complex Ki 10 μM. FJ9 binds ligand-binding pockets of NHERF1 PDZ domains to block cognate ligand interactions, disrupts Frizzled-7-Dishevelled interactions, and down-regulates canonical Wnt signaling. FJ9 induces apoptosis in cancer cells with intact β-catenin signaling. FJ9 can be used for the research of non-small cell lung cancer, melanoma .
|
-
- HY-181080
-
|
|
Topoisomerase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
TOP1/TDP1-IN-1 is a DNA topoisomerase 1B (TOP1) and tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitor with a TDP1 IC50 of 17.8 μM. TOP1/TDP1-IN-1directly suppresses TOP1 catalytic activity without forming a DNA-TOP1 ternary complex, inhibits TDP1-mediated repair of TOP1-induced DNA damage, and exhibits low acute toxicity. TOP1/TDP1-IN-1 disrupts DNA repair pathways, induces apoptosis, suppresses clonogenic growth, and elicits antiproliferative effects in cancer cells. TOP1/TDP1-IN-1 can be used for the research of non-small cell lung cancer, cervical cancer, colon cancer .
|
-
- HY-161885
-
|
|
SWI/SNF Complex
|
Cancer
|
|
SMARCA2-IN-6 is a SMARCA2 and SMARCA4 inhibitor, with an IC50 value of <0.005 μM for both SMARCA2 and SMARCA4. SMARCA2-IN-6 exerts anticancer activity against BRG1-mutant melanoma. SMARCA2-IN-6 can be used for research related to Brg1/Smarca4-mutant cancers .
|
-
- HY-171821
-
|
SGN-PDL1V
|
Antibody-Drug Conjugates (ADCs)
PD-1/PD-L1
|
Cancer
|
|
PF-08046054 (SGN-PDL1V) is a PD-L1-directed Antibody-drug conjugate (ADC), which is comprised of an anti-PD-L1 antibody conjugated to VcMMAE (HY-15575). PF-08046054 is direct cytotoxicity to PD-L1-expressing tumor cells via the intracellular delivery of MMAE. PF-08046054 can be used for the study of solid tumors
|
-
- HY-P11405
-
|
|
Neurotensin Receptor
|
Neurological Disease
Cancer
|
|
[D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P is a potent inhibitor of cell growth in small cell lung cancer (SCLC). [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P is also a neuropeptide antagonist, capable of blocking colony formation stimulated by various neuropeptides (including vasopressin and bradykinin). [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P inhibits the mobilization of Ca 2+ and the activation of mitogen-activated protein kinases induced by vasopressin or bradykinin. [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P inhibits the growth of H-69 xenograft tumors in nude mice .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-171821
-
|
SGN-PDL1V
|
Fluorescent Dyes
|
|
PF-08046054 (SGN-PDL1V) is a PD-L1-directed Antibody-drug conjugate (ADC), which is comprised of an anti-PD-L1 antibody conjugated to VcMMAE (HY-15575). PF-08046054 is direct cytotoxicity to PD-L1-expressing tumor cells via the intracellular delivery of MMAE. PF-08046054 can be used for the study of solid tumors
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-156002
-
|
Paluratide
|
Ras
ERK
|
Cancer
|
|
LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer .
|
-
- HY-164388
-
|
|
Caspase
Apoptosis
Autophagy
Necroptosis
|
Cardiovascular Disease
Cancer
|
|
Z-VAD is an irreversible, broad-spectrum pan-caspase inhibitor that can inhibit a variety of caspases including caspase-3, -6, -7, -8, -9, etc. (with a weaker inhibitory effect on caspase-2). Z-VAD can block apoptosis signaling pathways, induce autophagy and necrosis in tumor cells, and has anti-angiogenic activity. Z-VAD can enhance the sensitivity of breast cancer and lung cancer cells to radiotherapy in vitro and in vivo, and prolong the growth delay of tumor xenograft models. Z-VAD is well tolerated and is mainly used in research related to cancer radiosensitization and cell death pathway regulation .
|
-
- HY-P10759
-
|
|
Peptide-Drug Conjugates (PDCs)
Aminopeptidase
|
Cancer
|
|
DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
|
-
- HY-P10988
-
|
|
Apoptosis
MDM-2/p53
Integrin
|
Cancer
|
|
LVTX-8 is a peptide toxin, exacted from Lycosa vittata. LVTX-8 has potent anticancer and and anti-metastasis activities towards lung cancer with strong cytotoxicity. LVTX-8 significantly induces apoptosis and inhibits the proliferation, invasion and migration of lung cancer cells through P53 hypoxia pathways and integrin signaling. LVTX-8 significantly inhibits the tumor growth and metastasis in A549/H460 xenograft mice model .
|
-
- HY-P11405
-
|
|
Neurotensin Receptor
|
Neurological Disease
Cancer
|
|
[D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P is a potent inhibitor of cell growth in small cell lung cancer (SCLC). [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P is also a neuropeptide antagonist, capable of blocking colony formation stimulated by various neuropeptides (including vasopressin and bradykinin). [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P inhibits the mobilization of Ca 2+ and the activation of mitogen-activated protein kinases induced by vasopressin or bradykinin. [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P inhibits the growth of H-69 xenograft tumors in nude mice .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P99275
-
|
AMG-888; U3-1287
|
EGFR
Akt
ERK
PARP
Survivin
|
Cancer
|
|
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
|
-
(5)
-
- HY-P9964
-
|
11F8; IMC-11F8; LY3012211
|
EGFR
|
Cancer
|
|
Necitumumab (11F8; IMC-11F8; LY3012211) is a human IgG monoclonal antibody directed against EGFR. Necitumumab binds to the EGF binding site of EGFR, blocks ligand binding, neutralizes ligand-induced EGFR phosphorylation and downstream signaling, induces EGFR internalization and degradation, and mediates antibody-dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells. Necitumumab enhances antitumour activity in combination with Gemcitabine (HY-17026) and Cisplatin (HY-17394) in murine non-small-cell lung cancer xenograft models. Necitumumab can be used in research on cancers such as non-small cell lung cancer and colorectal cancer .
|
-
(5)
-
- HY-P99364
-
|
Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1
|
VEGFR
Apoptosis
p38 MAPK
Akt
|
Endocrinology
Cancer
|
|
Icrucumab (Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1) is an IgG1 antibody inhibitor targeting VEGFR-1/FLT1 with anti-tumor activity. By blocking ligand-dependent phosphorylation and downstream signal transduction, Icrucumab reduces the activities of MAPK and Akt in breast cancer xenograft models, inhibits the proliferation and invasion of VEGFR-1-positive tumor cells, and reverses the conversion of M1 macrophages to the pro-tumor M2-like phenotype. Icrucumab also inhibits tumor cell proliferation, promotes apoptosis, and effectively suppresses tumor growth through direct targeting of tumors and host support mechanisms. In addition, Icrucumab exhibits a synergistic effect when combined with chemotherapeutic agents, and it is used in research related to various cancers including advanced solid malignancies, thyroid cancer, melanoma, and lung cancer .
|
-
(5)
-
- HY-P99866
-
|
MEHD-7945A; RG 7597
|
EGFR
Akt
p38 MAPK
Apoptosis
|
Cancer
|
|
Duligotuzumab (MEHD-7945A; RG 7597) is a humanized IgG-κ monoclonal antibody targeting EGFR. Duligotuzumab blocks the binding of ligands to these two receptors, inhibits downstream HER/ErbB, AKT and MAPK signaling pathways, induces antibody-dependent cellular cytotoxicity, reduces the proliferation and migration abilities of cancer cells, promotes apoptosis, exerts radiosensitizing effects, and reverses EGFR resistance in cancer cells. Duligotuzumab can be used in tumor-related research .
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-
(5)
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- HY-P99943
-
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KN-046
|
PD-1/PD-L1
CTLA-4
|
Cancer
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Erfonrilimab (KN-046) is a monoclonal antibody targeting PD-L1/CTLA-4. Erfonrilimab blocks the PD-L1 and CTLA-4 pathways, thereby regulating T cell function. Erfonrilimab enhances the secretion of IL-2 in superantigen-stimulated peripheral blood mononuclear cells. Erfonrilimab inhibits tumor growth in xenograft and double gene knock-in mouse models. Erfonrilimab can be used in research related to a variety of advanced solid tumors, including non-small cell lung cancer and nasopharyngeal carcinoma.
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(5)
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- HY-P991669
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AML-01
|
Caspase
Apoptosis
|
Cancer
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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. .
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(5)
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- HY-P990947
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AZD9592 Antibody
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ADC Antibody
EGFR
|
Cancer
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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) .
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(5)
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- HY-P990953
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Gen1047
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CD3
|
Cancer
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Zubotamig (Gen1047) is an CD3E/VTCN1-targeting Ig(G1 -κ_G1 -λ2) type chimeric human antibody. The recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001). Zubotamig induces T-cell mediated cytotoxicity of B7H4-positive tumor cells, triggers T-cell activation, and induces cytokine release from T cells in the presence of B7H4-expressing tumor cells. Zubotamig demonstrates antitumor activity in mouse patient-derived xenograft (PDX) models. Zubotamig can be used for the research of solid cancers (including breast, ovarian and lung cancer) .
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(5)
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- HY-P992158
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CD47
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Cancer
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VBI-009 is a CD47 and B7-H3 (CD276) bispecific antibody. VBI-009 blocks CD47-SIRPα 'don't eat me' signals and restricts activity to CD47 +/B7-H3 + cells. VBI-009 induces antibody-dependent cellular phagocytosis (ADCP) and antibody-dependent cellular cytotoxicity (ADCC) in CD47 +/B7-H3 + tumor cells. VBI-009 inhibits tumor growth in CD47+/B7-H3+ lung cancer xenograft models. VBI-009 can be used for the research of lung cancer .
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(5)
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- HY-P992338
-
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Mesothelin
Constitutive Androstane Receptor
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Inflammation/Immunology
Cancer
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CT-1119 is an autologous human anti-Mesothelin chimeric antigen receptor macrophage (CAR-M). CT-1119 mediates CAR-dependent, antigen-dependent functional activities. CT-1119 acts as a phagocytosis inducer, tumor cell killer, pro-inflammatory cytokine inducer, and M1 macrophage polarizer. CT-1119 exhibits stronger resistance to M2 repolarization and reduces tumor burden in a mouse lung cancer xenograft model. CT-1119 can be used for the research of mesothelin-expressing solid tumors .
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(5)
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- HY-P991999
-
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FGFR
IFNAR
Interleukin Related
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Cancer
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OM-RCA-01 is an anti-FGFR1 monoclonal antibody with a Kd of 1.59 nM for human FGFR1. OM-RCA-01 inhibits the phosphorylation of FGFR1, blocks FGF-mediated signaling pathways, and suppresses the proliferation of downstream tumor cells. OM-RCA-01 delays tumor growth in lung cancer and renal cancer xenograft models expressing FGFR1. When combined with Nivolumab, OM-RCA-01 enhances the release of IFN-γ and IL-2. OM-RCA-01 is applicable for the research of lung cancer and renal cell carcinoma .
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(5)
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- HY-P992341
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MMP
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Cancer
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D8P1C1 is a high-affinity ADAM17 inhibitor (with a Kd of 180 pM targeting ADAM17-ECD) that reduces the shedding and phosphorylation of EGFR ligands. D8P1C1 inhibits cancer cell proliferation in vitro and tumor growth in xenograft models. 89Zr-DFO-D8P1C1 radioimmunological PET imaging shows its substantial accumulation in ovarian tumor xenografts, serving as a platform for generating bispecific T-cell engager derivatives. D8P1C1 can be applied to research on related diseases including triple-negative breast cancer, various types of ovarian cancer, lung adenocarcinoma, glioma, and colon cancer .
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-
(5)
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- HY-P992146
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MYTX-011 Antibody; Q-397
|
ADC Antibody
c-Met/HGFR
|
Cancer
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Zevontabart (MYTX-011 Antibody; Q-397) is a pH-dependent anti-c-MET antibody. Zevontabart regulates the trafficking process of c-MET to reduce receptor recycling, and enhances its own endocytosis and accumulation in c-MET-expressing cells. Zevontabart induces cytotoxicity in solid tumor cells and exerts anti-tumor activity in a non-small cell lung cancer xenograft mouse model. Zevontabart can be used to synthesize ADC, such as: MYTX-011. Zevontabart can be used in studies related to non-small cell lung cancer, with its corresponding isotype control being Human IgG1 kappa, Isotype Control (HY-P99001) .
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(5)
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- HY-P991967
-
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MAB100 Antibody
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EGFR
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Cancer
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AVID100 (MAB100) Antibody is a monoclonal antibody inhibitor targeting EGFR, which can be used to synthesize a novel antibody-drug conjugate (ADC) molecule AVID100. AVID100 Antibody is applicable to relevant research on breast cancer, head and neck cancer, and lung cancer .
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(5)
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- HY-P992163
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Fc Receptor (FcR)
C-type Lectin-like Receptors (CTLRs)
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Inflammation/Immunology
Cancer
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23ME-01473 is an anti-ULBP6/2/5 antibody with enhanced Fc effector function, with a Kd of 0.053 nmol/L against hULBP6, 0.23 nmol/L against hULBP2, and 1.92 nmol/L against hULBP5. 23ME-01473 restores anti-tumor immunity by activating NKG2D and FcγRIIIa. 23ME-01473 exerts anti-cancer activity in non-small cell lung cancer PDX models. 23ME-01473 can be used for the research of non-small cell lung cancer .
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(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0841
-
-
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- HY-N3980
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Guaiol
1 Publications Verification
Champacol; Guaiac alcohol
|
Infection
Structural Classification
Classification of Application Fields
Terpenoids
Sesquiterpenes
Distemonanthus benthamianus Baill.
Plants
Compositae
Disease Research Fields
Source Classification
|
Autophagy
RAD51
|
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Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
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- HY-N7694
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-
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- HY-N2199
-
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Structural Classification
Flavonoids
Classification of Application Fields
Phenols
Polyphenols
Selaginellaceae
Plants
Biflavones
Selaginella tamariscina (P. Beauv.) Spring
Disease Research Fields
Source Classification
Cancer
|
Apoptosis
Autophagy
PI3K
JNK
mTOR
p38 MAPK
CDK
MMP
TGF-beta/Smad
STAT
β-catenin
Reactive Oxygen Species (ROS)
Bcl-2 Family
Caspase
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Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits phosphorylation of PI3K, Akt, mTOR, JNK, and p38 MAPK; modulates expression of Cyclin D1, CDK4, Bcl-2, Bax, cleaved caspases 3/9, MMP-9, TGF-β, STAT3, and β-catenin. Sotetsuflavone induces G0/G1 cell cycle arrest, apoptosis, autophagy, and intracellular ROS elevation, inhibits cancer cell proliferation. Sotetsuflavone inhibits tumor growth in mouse tumor xenograft models. Sotetsuflavone can be used for the research of non-small cell lung cancer and Crohn’s disease .
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-
-
- HY-N3980R
-
|
Champacol (Standard); Guaiac alcohol (Standard)
|
Structural Classification
Natural Products
Distemonanthus benthamianus Baill.
Plants
Compositae
Source Classification
|
Reference Standards
Autophagy
RAD51
|
|
Guaiol (Standard) is the analytical standard of Guaiol. This product is intended for research and analytical applications. Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
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-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-175318S
-
|
|
|
p53 Activator 15 is an orally active p53 Y220C activator. p53 Activator 15 enhances the DNA binding of p53 Y220C (SC50 = 0.58 nM) and significantly inhibits NUGC-3 cell proliferation. p53 Activator 15 effectively inhibits tumor growth in NUGC-3 xenograft mouse and rat models. p53 Activator 15 can be used to study gastric cancer .
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-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-157411
-
|
|
|
Alkynes
|
|
anti-TNBC agent-5 (compound 10C) is a triple-negative breast cancer (TNBC) inhibitor with good stability and pharmacokinetic properties. anti-TNBC agent-5 exhibits antiproliferative activity against a variety of cancer cells. anti-TNBC agent-5 can also effectively inhibit TNBC lung metastasis activity in the MDA-MB-231 xenograft model. anti-TNBC agent-5 can be used in cancer research .
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-
- HY-180200
-
|
|
|
Alkynes
|
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RNK08954 is an orally active KRASG12D inhibitor with a Kd of 0.0395 nM. RNK08954 selectively binds the inactive GDP-bound KRASG12D form, suppresses downstream KRAS-mediated signaling pathways p-ERK1/2 experssion. RNK08954 inhibits KRASG12D-mutant cell proliferation, induces G0-G1 cell cycle arrest, and inhibits tumor growth in mouse xenograft models. RNK08954 can be used for the research of non-small cell lung cancer, pancreatic ductal adenocarcinoma .
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