您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Cobimetinib hemifumarate
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:
 
Cobimetinib hemifumarate
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。
CAS NO:1369665-02-0
包装:500 mg
市场价:16491元

产品介绍
Cobimetinib hemifumarate 是一种有效的具有选择性的MEK1抑制剂,能够抑制MEK1的活性,IC50值为 4.2 nM。

产品描述

Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC 50 value against MEK1 is 4.2 nM.

体外活性

The EC 50 values of Cobimetinib (GDC-0973) for 888MEL and A2058 cells are 0.2 μM, 10 μM, respectivelly. Melanoma cells are treated with EC 50 concentration of MEK and PI3K inhibitors for 24 hours (888MEL: 0.05 μM GDC-0973, 2.5 μM GDC-0941; A2058: 2.5 μM GDC-0973, 2.5 μM GDC-0941) [1]. Mitochondrial OXPHOS limits cell death induced by cobimetinib (100 nM) in melanoma with constitutive MAPK activation in A375 cells [4].

体内活性

In the NCI-H2122 KRASG12C mutant non-small cell lung carcinoma (NSCLC) xenograft model, treatment with up to 5 mg/kg Cobimetinib (GDC-0973) lead to moderate TGI and at 10 mg/kg approaches tumor stasis [1]. GDC-0973 and GDC-0941 are administered to A2058 tumor-bearing mice daily (QD) or every third day (Q3D) either as single agents or in combination. The population rate constants associated with tumor growth inhibition for GDC-0973 and GDC-0941 are 0.00102 and 0000651 μM -1 h -1, respectively [2]. Following single doses of GDC-0973 (1, 3, or 10 mg/kg, p.o.) estimated in vivo IC 50 values of %pERK decrease based on tumor concentrations in xenograft mice are 0.78 (WM-266-4) and 0.52 μM (A375) [3].

Cas No.

1369665-02-0

分子式

C25H25F3IN3O6

分子量

589.25

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years