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CAS No. : 1001917-37-8
MCE 国际站:MK-8033
产品活性:MK-8033 是一种具有口服活性的 ATP 竞争性 c-Met/Ron 双重抑制剂 (IC50s: 1 nM (c-Met),7 nM (Ron)),优先结合活化的激酶构象 (activated kinase conformation)。MK-8033 可用于癌症的研究,例如乳腺癌,膀胱癌、非小细胞肺癌 (NSCLC)。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:c-Met/HGFR
In Vitro: MK-8033 (Compound 11r, 10 μM) displayed 31% inhibition of CYP3A4 (cytochrome P450 3A4).
MK-8033 (1 μM, 2 h) inhibits phosphorylation of Y1349 of c-Met (IC50: 0.03 μM) in the c-Met dependent gastric cancer cell line GTL-16.
MK-8033 (1-10 μM, 72 h) inhibits GTL-16 cell proliferation (IC50: 0.58 μM).
MK-8033 binds more tightly to phosphorylated c-Met (Kd: 3.2 nM) than to its unphosphorylated counterpart (Kd: 10.4 nM), and inhibits oncogenic c-Met activation loop mutants with IC50s ranging from 0.6 to 1 nM.
MK-8033 (0.1-10 μM, 2 h) reduces the phosphorylation of c-Met, ERK, and Akt in EBC-1 and H1993 cells.
MK-8033 (1 μM, 1 h) sensitizes EBC-1 and H1993 cells (high c-Met-expressing) to radiation.
MK-8033 (10 μM, 6 h) enhances γ-H2Ax levels in A549 cells compared to double irradiation and decreases in DNA repair.
MK-8033 (2 μM, 72 h) results in reduced cell proliferation, but modest induction of apoptosis in G-alpha protein mutant UM (uveal melanoma) cells.
In Vivo: MK-8033 (Compound 11r, oral administration, 3-100 mg/kg, twice daily for 21 days) inhibits tumor growth in GTL-16 c-Met amplified gastric tumor xenografts.
MK-8033 exhibits moderate clearance (t1/2: 0.8 h for rats, 3.1 h for dog) and favorable bioavailability (35% for rats, 33% for dog).
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Orally Active Compound Library | Chemical Probe Library | Anti-Lung Cancer Compound Library | Angiogenesis-Related Compound Library | Anti-Liver Cancer Compound Library | Anti-Colorectal Cancer Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | AMG-208 | DS-1205b free base | c-Met-IN-1 | Glumetinib | Savolitinib | c-Met-IN-11 | ABN401 | Foretinib | Bafisontamab | MK-2461 | Dalmelitinib | MK-8033 hydrochloride | c-Met-IN-12 | MET kinase-IN-4 | Telisotuzumab vedotin | Cabozantinib | AC-386 | c-Met inhibitor 1 | Pamufetinib | Mefatinib-d6 | Tyrosine kinase-IN-4 | PHA-665752 | JNJ-38877618 | SU11274 | AMG-458 | SCR-1481B1 | c-Met-IN-2 | Cabozantinib-d4
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