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subcutaneous xenograft models

" in MedChemExpress (MCE) Product Catalog:

21

Inhibitors & Agonists

5

Peptides

2

Inhibitory Antibodies

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-156618

    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-P9992

    BAY-2315497; PSMA-TTC

    PSMA Apoptosis Cancer
    Peligifatamab is a PSMA-targeted α-radioimmunoconjugate with an EC50 of 1.2 nM against human targets. Peligifatamab induces DNA damage, DNA double-strand breaks, cell cycle arrest and apoptosis (Apoptosis) in PSMA-positive prostate cancer cells. Peligifatamab reduces cell viability in a manner dependent on cellular PSMA expression levels. Peligifatamab inhibits tumor growth and tumor-induced abnormal bone growth in prostate cancer bone metastasis models. Peligifatamab exhibits antitumor efficacy in subcutaneous prostate cancer models and xenograft models. Peligifatamab can be used for the research of metastatic castration-resistant prostate cancer .
    Pelgifatamab
  • HY-120692

    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-P99925

    REGN421

    Notch Metabolic Disease Cancer
    Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
    Enoticumab
  • HY-155079

    EGFR Cancer
    DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models .
    DZD1516
  • HY-153190
    W1131
    1 Publications Verification

    Oxidative Phosphorylation STAT Ferroptosis Cancer
    W1131 is a potent STAT3 inhibitor, triggering ferroptosis. W1131 suppresses cancer progression in gastric cancer cell subcutaneous xenograft model, organoids model, and PDX model. W1131 effectively alleviates chemical resistance of cancer cells to 5-FU (HY-90006). W1131 regulates cell cycle, DNA damage response, and oxidative phosphorylation, including IL6-JAK-STAT3 pathway and ferroptosis pathway .
    W1131
  • HY-174984

    p97 Caspase p62 Cancer
    VCP/p97 IN-3 is a VCP/p97 allosteric inhibitor. VCP/p97 IN-3 shows the inhibitory activity against the VCP proteins with an IC50 of 9 nM and the mutant VCP proteins with IC50 of 12 nM (N660K) and 19 nM (V474A/D649A). VCP/p97 IN-3 increases K48-linked ubiquitination and the level of cleaved caspase-3. VCP/p97 IN-3 activates ER-stress and the UPR. VCP/p97 IN-3 inhibits tumor growth in RPMI-8226 cell subcutaneous xenograft mouse models. VCP/p97 IN-3 can be used for the study of multiple myeloma .
    VCP/p97 IN-3
  • HY-P5520

    Bombesin Receptor Radionuclide-Drug Conjugates (RDCs) Cancer
    GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects .
    GB-6
  • HY-146615

    TAM Receptor Cancer
    Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model .
    Axl-IN-6
  • HY-153190A
    W1131 TFA
    1 Publications Verification

    Ferroptosis STAT Cancer
    W1131 TFA is a potent STAT3 inhibitor that induces ferroptosis. W1131 inhibits cancer progression in subcutaneous xenograft, organoid, and PDX models of gastric cancer. W1131 effectively alleviates cancer cell chemoresistance to 5-FU (HY-90006). W1131 regulates the cell cycle, DNA damage response, and oxidative phosphorylation, including the IL6-JAK-STAT3 pathway and the ferroptosis pathway .
    W1131 TFA
  • HY-159937

    Wee1 CDK Cancer
    PKMYT1-IN-7 (compound 7) is an orally active PKMYT1 inhibitor with IC50 values of 1.6 nM and 0.06 μM against of PKMYT1 and pCDK1, respectively. PKMYT1-IN-7 suppresses the phosphorylation of CDK1 at T14 and Y15. PKMYT1-IN-7 shows anticancer activity both < and < .
    PKMYT1-IN-7
  • HY-175542

    STAT Apoptosis Reactive Oxygen Species (ROS) PARP Cancer
    KB-15 is a STAT3 inhibitor. KB-15 exhibits potent anti-proliferative activity against AGS gastric cancer cells (IC50 = 0.29 μM) and BGC-823 gastric cancer cells (IC50 = 0.65 μM). KB-15 exerts anti-tumor effects by inhibiting STAT3 phosphorylation, downregulating HO-1 expression, and promoting intracellular ROS accumulation. KB-15 induces G0/G1 phase cell cycle arrest and apoptosis, as well as suppresses colony formation and migration of gastric cancer cells. KB-15 demonstrates excellent anti-tumor efficacy in BGC-823 subcutaneous xenograft model. KB-15 can be used for the study of gastric cancer .
    KB-15
  • HY-163507

    Anaplastic lymphoma kinase (ALK) Cancer
    ALK5-IN-79 (compound 57) is an ALK inhibitor with anticancer activity, by blocking TGF-β1/SMAD signaling pathway. ALK5-IN-79 attenuates the production of extracellular matrix (ECM) and deposition of collagen. ALK5-IN-79 exhibits adequate pharmacokinetic (PK) properties and good in vivo tolerance.
    ALK5-IN-79
  • HY-P11618

    Glycoprotein VI Cancer
    10P3Me is a Glypican-3 (GPC3)-targeting probe with a Ka of 93.8 nM for the human target. 10P3Me exhibits high binding affinity to GPC3, targets GPC3-positive cells, and serves as an agent for PET imaging. 10P3Me selectively accumulates in GPC3-positive tumor tissues, including subcutaneous xenograft models and orthotopic HepG2-LUC liver cancer models, to achieve precise localization of lesions .
    10P3Me
  • HY-184290

    Neurological Disease Cancer
    PRMT5-IN-56 is a PRMT5⋅MTA complex inhibitor with an IC50 of 0.2 nM, oral activity, and blood-brain barrier penetration. PRMT5-IN-56 inhibits PRMT5 methyltransferase activity in an MTA-cooperative manner, suppresses symmetrical dimethylarginine levels in MTAP-deficient cells. PRMT5-IN-56 suppresses proliferation of MTAP-deleted cancer cells with high selectivity over MTAP-wild type cells. PRMT5-IN-56 induces dose-dependent tumor growth inhibition in subcutaneous xenograft models, inhibits intracranial tumor progression, and prolongs survival in orthotopic brain xenograft models. PRMT5-IN-56 exhibits high intrinsic permeability, good oral bioavailability, and a high brain-to-plasma ratio. PRMT5-IN-56 can be used for the research of MTAP-deleted cancers and glioblastoma .
    PRMT5-IN-56
  • HY-181675

    Microtubule/Tubulin Apoptosis Bcl-2 Family Caspase Cancer
    CHNQD-01522 is a microtubule inhibitor targeting the colchicine binding site on β-tubulin. CHNQD-01522 binds to the colchicine binding site on β-tubulin, inhibits microtubule polymerization, and evades P-glycoprotein transport in cancer cells. CHNQD-01522 inhibits proliferation, suppresses tumor cell colony formation, arrests cell cycle in G2/M phases, and induces apoptosis in cancer cells. CHNQD-01522 upregulates of Bax and activation of caspase-9 and caspase-3. CHNQD-01522 shows anti-tumor efficacy in subcutaneous and orthotopic hepatocellular carcinoma xenograft tumor models. CHNQD-01522 can be used for the research of hepatocellular carcinoma .
    CHNQD-01522
  • HY-186045

    Histone Methyltransferase Apoptosis DNA/RNA Synthesis ATP-binding cassette (ABC) transporters Cancer
    SKLB06489 is a selective and orally active inhibitor of type I PRMT enzymes, with IC50 values of 64.55 nM (PRMT1), 4.21 nM (PRMT6), and 51.27 nM (PRMT8). SKLB06489 inhibits cell proliferation, colony formation, DNA replication, and DNA damage repair in cancer cells. SKLB06489 induces G0/G1-phase cell cycle arrest and apoptosis in cancer cells. SKLB06489 enhances intracellular cholesterol efflux via ABCA1 and ABCG1 upregulation, disrupts cholesterol metabolic homeostasis, and suppresses tumor growth in subcutaneous xenograft models. SKLB06489 can be used for the research of triple-negative breast cancer (TNBC) .
    SKLB06489
  • HY-P11816

    Radionuclide-Drug Conjugates (RDCs) Cancer
    DOTA-cTMTP1 is a cyclic tumor-homing peptide precursor molecule. DOTA-cTMTP1 selectively binds to XPNPEP2 on highly metastatic tumor cells, accumulates and retains in hepatocellular carcinoma tumors, and maintains a high tumor-to-liver contrast over time in small animal models. After radiolabeling with 68Ga, DOTA-cTMTP1 forms a PET probe for positron emission tomography (PET) imaging of hepatocellular carcinoma (HCC).
    DOTA-cTMTP1
  • HY-181514

    STAT CDK c-Myc Apoptosis Cancer
    STAT3-IN-53 (Compound L20) is a STAT3 inhibitor with a Kd value of 6.16 μM. STAT3-IN-53 binds directly to the SH2 domain of STAT3, inhibits phosphorylation at the Y705 site without affecting the total STAT3 protein level, and suppresses the IL-6/JAK/STAT3 pathway. STAT3-IN-53 downregulates the transcription and expression of cyclin-D1 and c-Myc. STAT3-IN-53 induces cell cycle arrest and promotes Apoptosis. STAT3-IN-53 exhibits anticancer activity against colorectal cancer .
    STAT3-IN-53
  • HY-P11858

    ROR Radionuclide-Drug Conjugates (RDCs) Cancer
    DP1 peptide is a high-affinity ROR1-binding peptide with a Kd value of 74.9 nM. When labeled with 68Ga, DP1 peptide serves as a PET imaging agent, which features rapid tumor uptake, favorable target-to-nontarget ratios in various tumor models, and renal clearance, enabling non-invasive quantitative visualization of ROR1 expression. DP1 peptide can be used in research related to melanoma, hepatocellular carcinoma, colorectal cancer, and non-small cell lung cancer .
    DP1 peptide
  • HY-P11814

    Cyclic TMTP1

    Radionuclide-Drug Conjugates (RDCs) Drug Derivative Cancer
    cTMTP1 (Cyclic TMTP1) is the cyclic form of TMTP1 (HY-P11815). TMTP1 is a tumor-targeting peptide that selectively targets highly metastatic tumor cells. The cTMTP1-based [ 68Ga]Ga-DOTA-cTMTP1 probe is used for visualization of hepatocellular carcinoma. cTMTP1 can form a 68Ga-DOTA radiotracer that accumulates in highly metastatic cervical cancer cells and is used for microPET tumor visualization. cTMTP1 is applicable to research related to hepatocellular carcinoma and cervical cancer .
    cTMTP1

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