Glumetinib (SCC244) 是一种高选择性、口服生物利用度、ATP 竞争性 c-Met 抑制剂，IC50 为0.42 nM。Glumetinib 对 c-Met 的选择性超过 312 种激酶，包括 c-Met 家族成员 RON 和高度同源的激酶 Axl、Mer、TyrO3。Glumetinib 具有抗肿瘤活性。
货号:ajcx38612
CAS:1642581-63-2
分子式:C21H17N9O2S
分子量：459.48
溶解度:DMSO : 41.67 mg/mL (90.69 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity[1].

Glumetinib (SCC244) (0-10 nM; 72 hours) elicits selective and profound effects against c-Met-driven cancer cell proliferation[1].Glumetinib (0-50 nM; 24 hours) induces G1-S phase cell-cycle arrest in c-Met-addicted human cancer cells[1].

Glumetinib (2.5-10 mg/kg; p.o.; once daily for 2-3 weeks) significantly inhibits c-Met-driven tumor growth in cancer CDX models[1].Glumetinib shows significant antitumor efficiency in NSCLC and HCC tumor PDX models with MET aberration[1].

[1]. Ai J, et al. Preclinical Evaluation of SCC244 (Glumetinib), a Novel, Potent, and Highly Selective Inhibitor of c-Met in MET-dependent Cancer Models. Mol Cancer Ther. 2018 Apr;17(4):751-762.