PHA-665752,477575-56-7

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PHA-665752

CAS No. : 477575-56-7

MCE 国际站：PHA-665752

产品活性：PHA-665752 是一种选择性的 ATP 竞争活性位点 c-Met 激酶抑制剂，K_i 为 4 nM，IC₅₀为 9 nM。PHA-665752 对 c-Met 的选择性比一组不同的酪氨酸和丝氨酸苏氨酸激酶高 50 倍。PHA-665752 诱导细胞凋亡和细胞周期阻滞，具有细胞还原性抗肿瘤活性。

研究领域：Protein Tyrosine Kinase/RTK  |  Autophagy  |  Apoptosis

作用靶点：c-Met/HGFR  |  Autophagy  |  Apoptosis

In Vitro: PHA-665752 is a potent and ATP-competitive inhibitor of c-Met kinase activity with a K_i of 4 nM and an IC₅₀ of 9 nM.
PHA-665752 exhibits >50-fold selectivity for c-Met enzyme compared with the majority of kinases evaluated.
PHA-665752 shows potent inhibition of c-Met RTK autophosphorylation in NIH3T3 cells engineered to express high levels of c-Met and hepatocyte growth factor (HGF).
PHA-665752 inhibits HGF-stimulated or constitutive phosphorylation of mediators of downstream of c-Met such as Gab-1, ERK, Akt, STAT3, PLC-γ, and FAK in multiple tumor cell lines.
PHA-665752 (0-1.25 μM; 18 hours) potently inhibits HGF and c-Met-driven phenotypes such as cell growth (proliferation and survival), cell motility, invasion, and/or morphology of a variety of tumor cells.
PHA-665752 (0-1.25 μM; 72 hours) induces apoptosis in both the presence and absence of HGF at concentrations that inhibited tyrosine phosphorylation of c-Met in GTL-16 cells.
PHA-665752 (0.0125-0.2 μM; 4 hours) potent inhibits HGF-induced c-Met phosphorylation in A549 cells.

In Vivo: PHA-665752 (7.5-30 mg/kg/day; i.v. ; for 9 days) exhibits statistically significant dose-dependent tumor growth inhibition of 68%, 39%, and 20% of vehicle control at the 30 mg/kg/day, 15 mg/kg/day, and 7.5 mg/kg/day doses, respectively.
PHA-665752 shows a potent cytoreductive activity in a gastric carcinoma xenograft model.

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