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tumor xenograft mice model

" in MedChemExpress (MCE) Product Catalog:

81

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1

Biochemical Assay Reagents

3

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10

Inhibitory Antibodies

1

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2

Click Chemistry

3

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-153306
    Zovegalisib
    1 Publications Verification

    RLY-2608

    		 PI3K Cancer
    Zovegalisib (RLY-2608) is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. Zovegalisib inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin .
    Zovegalisib
  • HY-148273
    Setidegrasib

    ASP-3082; KRAS G12D inhibitor 17

    		 PROTACs Ras ERK Akt Cancer
    Setidegrasib (KRAS G12D inhibitor 17, ASP3082) is a PROTAC KRAS degrader (DC50: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib suppresses p-ERK, p-AKT, p-S6 levels in AsPC-1 cells. Setidegrasib exhibits anti-tumor activity in various cancer xenograft models in mice. Setidegrasib can be used for the study of KRAS(G12D)-mutated solid tumors. (Blue: VHL ligase ligand (HY-168699); Black: linker (HY-168698); Pink: G12D ligand (HY-168700)) .
    Setidegrasib
  • HY-100591
    SirReal2
    2 Publications Verification

    		 Sirtuin Neurological Disease Inflammation/Immunology Cancer
    SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration .
    SirReal2
  • HY-156618
    Irpagratinib

    ABSK011

    		 FGFR Cancer
    Irpagratinib (ABSK011) is an orally active FGFR4 inhibitor (IC50<10 nM). Irpagratinib inhibits FGFR4 autophosphorylation and blocks signaling from FGFR4 to downstream pathway activation. Irpagratinib has shown high exposure in PK studies in mice, rats, and dogs, and also demonstrated antitumor activity in a subcutaneous xenograft tumor model .
    Irpagratinib
  • HY-123972
    SEC inhibitor KL-2
    1 Publications Verification

    KL-2

    		 DNA/RNA Synthesis Cancer
    SEC inhibitor KL-2 (KL-2), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-2 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 1.50 μM .
    SEC inhibitor KL-2
  • HY-120692
    Cyclanoline chloride

    		JAK STAT Apoptosis Cancer
    Cyclanoline chloride is an alkaloid. Cyclanoline chloride can be isolated from Fangji. Cyclanoline (chloride) inhibits the phosphorylation of JAK2 and STAT3, and induces Apoptosis. Cyclanoline chloride suppresses tumor growth in subcutaneous bladder cancer xenograft models of nude mice. Cyclanoline chloride reverses cisplatin resistance in bladder cancer cells and enhances the efficacy of Cisplatin (HY-17394). Cyclanoline chloride can be used for research related to bladder cancer .
    Cyclanoline chloride
  • HY-P991584
    HuGAL-FR21

    		FGFR Cancer
    HuGAL-FR21 is a humanized antiFGFR2IIIb IgG1 monoclonal antibody. HuGAL-FR21 can block the binding of FGF2, FGF7, and FGF10 to FGFR2IIIb and inhibit FGF-induced phosphorylation of FGFR2IIIb. HuGAL-FR21 can downregulate the expression of FGFR2 in SNU-16 cells. HuGAL-FR21 shows the significant anti-tumor activity in athymic nude mice bearing gastric cancer xenograft models. HuGAL-FR21 can be used for research on cancer such as gastric cancer .
    HuGAL-FR21
  • HY-139659
    ARD-61

    		PROTACs Androgen Receptor Progesterone Receptor Apoptosis Cancer
    ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    ARD-61
  • HY-W111581
    Copper(II) diethyldithiocarbamate
    1 Publications Verification

    Diethyldithiocarbamic acid copper salt

    		 Apoptosis Caspase Cancer
    Copper(II) diethyldithiocarbamate (Diethyldithiocarbamic acid copper salt) is a Copper(II) and diethyldithiocarbamate coordination polymer. Copper(II) diethyldithiocarbamate binds tightly to NPL4 and induces its aggregation, disrupting the p97-NPL4-UFD1 pathway. Copper(II) diethyldithiocarbamate causes ubiquitinated proteins accumulation and impairs waste proteins degradation, thus resulting in cell apoptosis. Copper(II) diethyldithiocarbamate inhibits tumor growth in MDA-MB-231 xenograft mice models. Copper(II) diethyldithiocarbamate can be used for the research of cancer, such as breast cancer .
    Copper(II) diethyldithiocarbamate
  • HY-P99744
    Modakafusp alfa

    TAK-573

    		 CD38 Inflammation/Immunology Cancer
    Modakafusp alfa (TAK-573) is a humanized, anti-CD38 IgG4 monoclonal antibody fused to 2 attenuated IFNα2b molecules, which delivers interferon-alpha to CD38-expressing cells. Modakafusp alfa has direct anti-proliferative activity on multiple myeloma (MM) cancer cells in vitro and induces robust and durable antitumor responses in MM xenograft tumor models. Modakafusp alfa in combination with anti-PD-1 antibodies induces immunomodulation and antitumor responses with good tolerance in mice .
    Modakafusp alfa
  • HY-172158
    ALKBH5-IN-5
    1 Publications Verification

    		 Anaplastic lymphoma kinase (ALK) Caspase Cancer
    ALKBH5-IN-5 is a highly selective ALKBH5 (IC50 = 0.62 μM, Kd = 804 nM). ALKBH5-IN-5 disrupts ALKBH5 binding to m 6A-RNA and 6mA-DNA substrates. ALKBH5-IN-5 promotes differentiation, induces apoptosis, cause G2-M phase arrest and exerts strong antiproliferative effects in cancer cells. ALKBH5-IN-5 reduces TACC3 and MYC protein levels and increases cleaved caspase-3 levels. ALKBH5-IN-5 exerts antitumor activity in tumor xenograft mice models. ALKBH5-IN-5 can be used for the research of acute myeloid leukemia .
    ALKBH5-IN-5
  • HY-P99922
    Encelimab

    		LAG-3 Cancer
    Encelimab is an anti-LAG3 antibody. Encelimab blocks the interaction between LAG-3 and MHC II, and enhances T-cell activation. Encelimab alone or in combination with an anti-PD-1 antibody reduces tumor size in a lymphoma mice model (A20 cell xenograft) .
    Encelimab
  • HY-149480
    ERD-3111

    		PROTACs Estrogen Receptor/ERR Cancer
    ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
    ERD-3111
  • HY-P991570
    Zaptuzumab

    AD5-10; oba-01 Antibody

    		 TNF Receptor Apoptosis Caspase Atg8/LC3 Akt Beclin1 JNK Cancer
    Zaptuzumab (AD5-10) is a DR5-specific humanized monoclonal antibody that selectively binds to DR5 with high affinity. Zaptuzumab specifically induces cancer cell death by both caspase-apoptosis and autophagic cell death (ACD). Zaptuzumab activates both ADCC and CDC. Zaptuzumab induces ROS generation and GSH level reduction. Zaptuzumab shows a significant suppression of the tumor growth and good safety in various xenografts mice tumor models .
    Zaptuzumab
  • HY-174346
    Skp2-IN-4

    		E1/E2/E3 Enzyme Apoptosis DNA/RNA Synthesis Cancer
    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 .
    Skp2-IN-4
  • HY-149862
    ARD-2051
    1 Publications Verification

    		 PROTACs Androgen Receptor Cancer
    ARD-2051 is a selective and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 exhibits effective anti-tumor activity in VCaP xenograft mice model. ARD-2051 can be used for the research of prostate cancer (Pink: AR ligand (HY-400666), Blue: CRBN Ligand (HY-14658), Black: Linker) .
    ARD-2051
  • HY-168035
    W4275

    		Histone Methyltransferase Cancer
    W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity, showing an IC50 value of 17 nM. W4275 exhibits antiproliferative activity with an IC50 of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research .
    W4275
  • HY-169120
    FKB04

    		Telomerase Cancer
    FKB04 is a telomeric repeat binding factor 2 (TRF2) inhibitor that exerts its antitumor activity by disrupting the telomere maintenance mechanism in liver cancer cells, leading to T-loop defects, telomere shortening, and cellular senescence. Additionally, FKB04 can inhibit tumor growth in a human liver cancer xenograft mouse model (with Huh-7 cells implanted in BALB/c mice). FKB04 can be used in liver cancer research .
    FKB04
  • HY-172930
    PVTX-405

    		Molecular Glues IKZF Family Potassium Channel Inflammation/Immunology Cancer
    PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC50  of  0.7 nM and a Dmax of 91%. PVTX-405 enhances degradation efficiency, significantly reduces off-target degradation, and alleviates hERG inhibition with IC50 of 48 µM. PVTX-405 significantly inhibits the growth of MC38 tumors, with greater synergistic anti-cancer efficacy in combination with immune checkpoint therapies (ICTs) (anti-PD1 or anti-LAG3) in the MC38 mouse tumor xenograft model using Crbn 391V C57BL/6 mice .
    PVTX-405
  • HY-174850
    CFON-026

    		Btk Cancer
    CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27  nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia .
    CFON-026
  • HY-171572
    Atezolizumab-MMAE

    		Antibody-Drug Conjugates (ADCs) Microtubule/Tubulin Apoptosis Inflammation/Immunology Cancer
    Atezolizumab-MMAE is an anti-PD-L1 antibody-drug conjugate (ADC) with an EC50 of 1.1 nM. Atezolizumab-MMAE is composed of a humanized anti-PD-L1 antibody (Atezolizumab) (HY-P9904), a lysosomally cleavable dipeptide linker (valine-citrulline), a tubulin inhibitor (MMAE) (HY-15162), and the drug-linker conjugate for ADC is VcMMAE (HY-15575). Atezolizumab-MMAE has a potent cytotoxicity (EC50: 9.75-11.94 nM) and immune activation effect. Atezolizumab-MMAE has a significantly anti-tumor activity in MC38 xenograft PD-1-humanized immune system mice model .
    Atezolizumab-MMAE
  • HY-155887
    DSPE-PEG-Amine, MW 3400 ammonium

    DSPE-PEG-NH2, MW 3400 ammonium

    		 Liposome Cancer
    DSPE-PEG-Amine (DSPE-PEG-NH2), MW 3400 ammonium is an amino-functionalized PEGylated phospholipid. It serves not only as a key component for preparing σ receptor-targeted liposomes (such as anisamide-modified lipids) but also as a starting material for synthesizing click chemistry- and tumor-targeted lipids including DSPE-PEG-DBCO (HY-155788) and DSPE-PEG2000-TCO (HY-170704). DSPE-PEG-Amine, MW 3400 ammonium effectively modulates the ζ potential of nanoparticles, enables complexation with nucleic acids or proteins to protect DNA from nuclease degradation, and supports ligand conjugation on the nanoparticle surface. It is used in studies related to DU-145 tumors, breast cancer, and other relevant research .
    DSPE-PEG-Amine, MW 3400 ammonium
  • HY-P991609
    ABX-MA1

    		MMP Cancer
    ABX-MA1 is a humanized IgG2 monoclonal antibody inhibitor targeting MCAM/MUC18. ABX-MA1 significantly decreases homotypic aggregation and heterotypic adhesion to HUVECs, and the formation of experimental lung metastasis. ABX-MA1 potently inhibits tumor growth, angiogenesis, and MMP-2 expression in A375SM/WM2664 xenograft mice model, promising for melanoma research .
    ABX-MA1
  • HY-P991571
    GC1118

    GC-1118A

    		 EGFR PERK Akt Cancer
    GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (KD) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer .
    GC1118
  • HY-W338346
    Salicylate choline

    		Drug Derivative Interleukin Related TNF Receptor Polo-like Kinase (PLK) Inflammation/Immunology Cancer
    Salicylate choline is an orally active derivative of Aspirin (acetylsalicylic acid) (HY-14654). Salicylate choline significantly reduces IL-1β, IL-6, TNF-α and IL-10 levels in cells. Salicylate choline enhances the anti-tumor activity of the CRM1 inhibitor Selinexor (KPT-330) (HY-17536) through inducing S-phase cell cycle arrest and impairing DNA damage repair. Salicylate choline combined with Selinexor demonstrates excellent anti-tumor efficacy in mice xenograft model harboring JeKo-1 cells. Salicylate choline can be used for the study of rheumatic diseases, inflammation and cancer .
    Salicylate choline
  • HY-174458
    MD-4251

    		PROTACs MDM-2/p53 IKZF Family Casein Kinase Cancer
    MD-4251 is an orally active MDM2 PROTAC degrader. MD-4251 potently degrades MDM2 in RS4;11 cells (DC50: 0.2 nM) and actives p53. MD-4251 shows strong antiproliferative activity against acute leukemia cells (wild-type p53) with minimal efficacy in mutant type. MD-4251 induces complete tumor regression in RS4;11 xenograft mice model . Pink: MDM2 ligand (HY-130684); Blue: CRBN ligase ligand (HY-W883326); Black: linker
    MD-4251
  • HY-176128
    BWA-6047

    		PROTACs Androgen Receptor Apoptosis PARP Caspase Cancer
    BWA-6047 is an oral active PROTAC degrader targeting AR/AR-V7 and GSPT1 with DC50 values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer .
    BWA-6047
  • HY-176239
    PROTAC PI3Kδ degrader-1

    		PROTACs PI3K Akt Apoptosis Autophagy Cancer
    PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ PROTAC degrader with a DC50 of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model . Pink: PI3Kδ ligand (HY-169983); Blue: VHL ligase ligand (HY-112078); Black: linker (HY-W013381)
    PROTAC PI3Kδ degrader-1
  • HY-153834
    GTI 2040

    		DNA/RNA Synthesis Cancer
    GTI-2040, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
    GTI 2040
  • HY-165421
    Mps1-IN-10

    		Mps1 Cancer
    Mps1-IN-10 (Compound 9) is an inhibitor for Mps1 with an IC50 of 6.4 nM. Mps1-IN-10 inhibits the proliferation of cancer cell MDA-MB-231 with a GI50 of 11 nM. Mps1-IN-10 exhibits anti-tumor efficacy in mice MDA-MB-231 xenograft models .
    Mps1-IN-10
  • HY-175342
    FCN-338

    LOXO-338

    		 Bcl-2 Family Cancer
    FCN-338 (LOXO-338) is an orally active and selective Bcl-2 inhibitor with an IC50 of 4.5 nM for Bcl-2/BAK interaction. FCN-338 potently inhibits tumor growth in follicular lymphoma (FL), acute myeloid leukemia (AML), and acute lymphoblastic leukemia (ALL) xenograft mice model without significant weight loss. FCN-338 has a broad-spectrum anti-cancer activity, such as FL, CLL/SLL, AML, and ALL .
    FCN-338
  • HY-178061
    APS03118

    		ERK RET Cancer
    APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research .
    APS03118
  • HY-165606
    SB-T-1214

    		Oct3/4 c-Myc Apoptosis Cancer
    SB-T-1214 (SBT) is a taxane. SB-T-1214 efficiently inhibits expression of stem cell-related genes (Oct4, Sox2, and c-Myc) and induces apoptosis of colon cancer spheroids with drug resistant tumorigenic CD133 +/CD44 + cells. SB-T-1214 strongly represses tumor growth in Pgp+ DLD-1 human colon tumor xenografts mice model. SB-T-1214 can be used for antitumor research, especially against tumors with drug resistance, such as colon, pancreatic and renal cancers .
    SB-T-1214
  • HY-176220
    GPX4-AUTAC

    		AUTACs Autophagy Glutathione Peroxidase Ferroptosis Cancer
    GPX4-AUTAC is a GPX4-targeting autophagy-mediated degrader (AUTAC). GPX4-AUTAC consists of an inhibitor ML162-yne (HY-153748), a degradation tag FBnG (HY-W073762) and a glycol linker (HY-W021401). GPX4-AUTAC promotes the ubiquitination of GPX4 by E3 ligase TRAF6, and enhances the binding with GPX4 and p62, leading to the selective autophagy-dependent degradation of GPX4. GPX4-AUTAC significantly induces ferroptosis and shows a potent anti-cancer activity in breast cancer cells, breast cancer-derived organoids (PDOs) and MDA-MB-231 tumor xenograft mice model, with potent synergistic effects when combined with Sulfasalazine (SAS) (HY-14655) or chemotherapy drugs (Paclitaxel (HY-B0015) or Cisplatin (HY-17394)) .
    GPX4-AUTAC
  • HY-178098
    TEAD-IN-21

    		YAP Cancer
    TEAD-IN-21 is a potent and orally active pan-TEAD inhibitor with an IC50 of 3 nM. TEAD-IN-21 effectively inhibited the proliferation of Huh-7 cells. TEAD-IN-21 selectively downregulates TEAD-dependent downstream genes. TEAD-IN-21 achieves tumor regression in a liver cancer-derived tumor xenograft mice model. TEAD-IN-21 can be used in the research of hepatocellular carcinoma (HCC) .
    TEAD-IN-21
  • HY-177270
    CHNQD-01281

    		EGFR Drug Derivative Cancer
    CHNQD-01281, a derivative of Brefeldin A (HY-16592), is a EGFR modulator. CHNQD-01281 has strong antiproliferative activities against cancer cells (IC50: 0.079 and 0.081 μM for T24 and J82 cells, respectively). CHNQD-01281 regulates both EGFR/PI3K/AKT and EGFR/ERK pathways and mediates the chemotactic effect of chemokines on immune effector cells. CHNQD-01281 remarkably inhibits tumor growth in T24 xenograft mice model and prolongs the survival time in MB49 allogeneic mice model via inducing infiltration of cytotoxic T cells .
    CHNQD-01281
  • HY-174847
    VCP/p97 IN-2

    		p97 Cancer
    VCP/p97 IN-2 (Compound V13) is a VCP/p97 inhibitor with IC50 of 32 nM for p97. VCP/p97 IN-2 has excellent antitumor activities and significantly inhibits tumor growth in Molm-13 xenograft mice model. VCP/p97 IN-2 can be used for acute myeloid leukemia (AML) research .
    VCP/p97 IN-2
  • HY-P10992
    YVPGP

    		PI3K Akt mTOR Caspase Apoptosis Bcl-2 Family Cancer
    YVPGP is an oligopeptide exacted from Anthopleura anjunae. YVPGP has a significant antitumor activity by mediating PI3K/AKT/mTOR signaling pathway. YVPGP arrests DU-145 cells in the S phase and induces apoptosis via mitochondrial and death receptor pathways (caspase3, 7, 8, 9). YVPGP effectively inhibits tumor growth in DU-145 xenografts mice model, promising for prostate cancer research .
    YVPGP
  • HY-P10988
    LVTX-8

    		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 .
    LVTX-8
  • HY-178008
    Mcl-1-IN-16

    		Bcl-2 Family Caspase Apoptosis Cancer
    Mcl-1-IN-16 is an effective macrocyclic myeloid cell leukemia 1 (Mcl-1) inhibitor with a Ki of below 0.08 nM. Mcl-1-IN-16 maintains high selectivity (>50,000-fold) for Mcl-1 over other antiapoptotic Bcl-2 family members Bcl-2 and Bcl-xL. Mcl-1-IN-16 leads to the activation of caspase-3/7, thereby initiating cell apoptosis. Mcl-1-IN-16 achieves tumor regression in a lung cancer-derived tumor xenograft mice model. Mcl-1-IN-16 can be used in the research of solid tumor such as nonsmall cell lung cancer (NSCLC) .
    Mcl-1-IN-16
  • HY-P991243
    MP-RM-1

    		EGFR Akt Cancer
    MP-RM-1 is an antibody-based, non-competitive ErbB-3 inhibitor with a Kd value of 32.7 nM. MP-RM-1 inhibits both ligand-dependent and ligand-independent ErbB-3 activation, blocks ErbB-2/ErbB-3 heterodimerization, induces ErbB-3 internalization and degradation, and suppresses the phosphorylation of downstream Akt. MP-RM-1 exerts its antagonistic effect through a non-competitive mechanism. MP-RM-1 inhibits tumor growth in melanoma and prostate cancer xenograft models in nude mice and reduces the proliferative activity of tumor cells .
    MP-RM-1
  • HY-148291
    BrP-LPA sodium

    		LPL Receptor Phosphodiesterase (PDE) Cancer
    BrP-LPA sodium is a pan-opposite agent for lysophosphatidic acid (LPA). It has antagonistic activity against LPA1 (IC50 = 4520 nM), LPA2 (IC50 = 468 nM), LPA3, and LPA4. BrP-LPA sodium also has partial agonistic activity for LPA5, with its EC50 being 1282 nM. BrP-LPA sodium has ATX inhibitory activity. BrP-LPA sodium effectively inhibits the migration and invasion of breast cancer cells. BrP-LPA sodium achieves tumor regression and anti-angiogenesis in mice breast cancer xenograft model. BrP-LPA sodium can be used for the study of breast cancer .
    BrP-LPA sodium
  • HY-177021
    Tubulin-IN-51

    		Microtubule/Tubulin Apoptosis Cancer
    Tubulin-IN-51 is an orally available, potent tubulin inhibitor (IC50 = 31 nM). Tubulin-IN-51 promotes tubulin polymerization in vitro and does not compete with Paclitaxel (HY-B0015) for binding. Tubulin-IN-51 inhibits the binding of Vinblastine (HY-13780) to tubulin. Tubulin-IN-51 downregulates the proportion of cells in the G1 phase and induces apoptosis. Tubulin-IN-51 inhibits tumor growth in multiple nude mouse xenograft models .
    Tubulin-IN-51
  • HY-156792
    RIOK2-IN-1

    		RIO Kinase Cancer
    RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression .
    RIOK2-IN-1
  • HY-174315
    WZH-17-002

    		PROTACs Anaplastic lymphoma kinase (ALK) Akt ERK Cancer
    WZH-17-002 is a WZH-15-125-based ALK PROTAC degrader with a DC50 of 25 nM. WZH-17-002 enhances activities against Lorlatinib (HY-12215)-resistant ALK compound mutations. WZH-17-002 significantly reduces drug resistance in ALK-fusion non-small cell lung cancer (NSCLC) and inhibits tumor growth in EML4-ALK G1202R/L1196 M xenograft mice model . Pink: ALK ligand (HY-174314); Blue: CRBN ligase ligand (HY-14658); Black: linker (HY-174316)
    WZH-17-002
  • HY-106159
    SB-T-101141

    		Reactive Oxygen Species (ROS) p38 MAPK JNK PERK Ferroptosis Cancer
    SB-T-101141 is a novel taxane. SB-T-101141 effectively induces a noncanonical ferroptosis to overcome Paclitaxel (HY-B0015) resistance of breast cancer. SB-T-101141 facilitates the production of iron and ferrous ions and ROS. SB-T-101141 stably binds to KHSRP to inhibit the iron-dependent expression of CISD1 related to iron homeostasis. SB-T-101141 synergistically enhances the iron-dependent activation of JNK and PERK pathways via KHSRP. SB-T-101141 suppresses breast tumor growth in MCF-7(PR)/MDA-MB-231(PR) or KHSRP knock-down MCF-7 xenograft mice model .
    SB-T-101141
  • HY-176225
    BY13

    		PROTACs Src Estrogen Receptor/ERR Apoptosis Cancer
    BY13 is a SRC-3 PROTAC degrader with a DC50 of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant (HY-13636). BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model . Pink: SRC-3 ligand (SI-2) (HY-101447); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-176226)
    BY13
  • HY-176288
    eIF4E/eIF4G PPI-IN-1

    		Eukaryotic Initiation Factor (eIF) Bcl-2 Family Apoptosis Ras PERK Cancer
    eIF4E/eIF4G PPI-IN-1 is an eIF4E/eIF4G interaction inhibitor with a KD of 20.2 μM for eIF4E protein. eIF4E/eIF4G PPI-IN-1 plays an antitumor role in multiple modes of action including regulating the activity of eIF4E by inhibiting the Ras/MAPK/eIF4E signaling pathway, apoptosis and cell migration. eIF4E/eIF4G PPI-IN-1 suppresses the growth of HepG2 xenografts in nude mice and was relatively nontoxic to mice .
    eIF4E/eIF4G PPI-IN-1
  • HY-174415
    ZSH-2117

    		PROTACs EGFR Akt ERK Cancer
    ZSH-2117 is a covalent and selective EGFR PROTAC degrader with a DC50 of 45 nM in Ba/F3-EGFR L858R/T790M/C797S cells. ZSH-2117 significantly inhibits cell proliferation and reduces the downstream EGFR signaling proteins level of AKT and ERK. ZSH-2117 effectively inhibits tumor growth in Ba/F3-EGFR L858R/T790M/C797S xenograft mice model . Pink: EGFR ligand (HY-175162); Blue: NEDD4 ligase ligand (HY-175159); Black: linker
    ZSH-2117
  • HY-175610
    PROTAC FLT3/JAK2/BRD4 Degrader-1

    		PROTACs FLT3 JAK Epigenetic Reader Domain Cancer
    PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)) .
    PROTAC FLT3/JAK2/BRD4 Degrader-1

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