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MK-8033 hydrochloride

CAS No. : 1283000-43-0

MCE 国际站：MK-8033 hydrochloride

产品活性：MK-8033 hydrochloride 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 hydrochloride 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 hydrochloride (Compound 11r, 10 μM) displayed 31% inhibition of CYP3A4 (cytochrome P450 3A4).
MK-8033 hydrochloride (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 hydrochloride (1-10 μM, 72 h) inhibits GTL-16 cell proliferation (IC₅₀: 0.58 μM).
MK-8033 hydrochloride binds more tightly to phosphorylated c-Met (K_d: 3.2 nM) than to its unphosphorylated counterpart (K_d: 10.4 nM), and inhibits oncogenic c-Met activation loop mutants with IC₅₀s ranging from 0.6 to 1 nM.
MK-8033 hydrochloride (0.1-10 μM, 2 h) reduces the phosphorylation of c-Met, ERK, and Akt in EBC-1 and H1993 cells.
MK-8033 hydrochloride (1 μM, 1 h) sensitizes EBC-1 and H1993 cells (high c-Met-expressing) to radiation.
MK-8033 hydrochloride (10 μM, 6 h) enhances γ-H2Ax levels in A549 cells compared to double irradiation and decreases in DNA repair.
MK-8033 hydrochloride (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 hydrochloride (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 hydrochloride exhibits moderate clearance (t_1/2: 0.8 h for rats, 3.1 h for dog) and favorable bioavailability (35% for rats, 33% for dog).

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