您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Glumetinib
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Glumetinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Glumetinib图片
CAS NO:1642581-63-2
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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。
Cas No.1642581-63-2
别名谷美替尼,SCC244
分子式C21H17N9O2S
分子量459.48
溶解度DMSO : 41.67 mg/mL (90.69 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.