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c-Met-IN-14

CAS No. : 2443380-34-3

MCE 站：c-Met-IN-14

产品活性：c-Met-IN-14 (compound 26af) 是 N- 磺酰胺基衍生物，是一种 c-Met 激酶抑制剂，IC₅₀ 为 2.89 nM。c-Met-IN-14 通过阻断 c-Met 的磷酸化表现出抗癌活性，并将细胞周期阻滞在 G2/M 期。c-Met-IN-14 呈剂量依赖性诱导 A549 细胞凋亡 (apoptosis)。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：c-Met/HGFR  |  c-Kit  |  FLT3  |  Apoptosis

In Vitro: c-Met-IN-14 (compound 26af) is a relatively selective inhibitor of c-Met kinase (IC₅₀=2.89 nM), because of high inhibitory effects against c-Kit (IC₅₀=4.26 nM) ａnd Flt-3 (IC₅₀=7.28 nM).
c-Met-IN-14 (0.28-0.72 μM; 24 h) exhibits the remarkable anti-proliferative activities against cancer cell lines (A549, HT-29, MKN-45 ａnd MDA-MB-231), with IC₅₀s of 0.28-0.72 μM.
c-Met-IN-14 (0.25, 0.5, ａnd 1.0 μM; 12 h) induces the late apoptotic ａnd early apoptotic ａnd (0.25, 0.5, ａnd 1.0 μM; 24 h) shows anti-proliferative of A549 cells by arresting cell cycle at G2/M phase ａnd apoptosis induction.
c-Met-IN-14 (1.35, or 6.12 μM, respectively; 24 h) has moderate selectivity towards cancer cells over normal cells, with the selectivity index of 4.2 ａnd 19.1 to HUVEC (IC₅₀=1.35 μM) ａnd FHC cells (IC₅₀=6.12 μM), respectively.

In Vivo: c-Met-IN-14 (compound 26af) (p.o.; 8 mg/kg) exhibits safety profile ａnd favorable pharmacokinetic properties in BALB/c mouse, with rapid absorption (T_max=2.5 h), high maximum concentration (C_max=1228.4 ng/mL), high plasma exposure (AUC_0-∞=6.8 g.h.mL^-1), accepted elimination half-life (T_1/2=3.5 h), ａnd well clearance (1.18 L.h_-1.kg_-1), has a moderate oral bioavailability (74%) in mouse.
c-Met-IN-14 (i.p.; below 200 mg/kg) doesn’t cause abnormalities, anaphylactic responses, allergic reactions on mice.

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