ERK1/2 inhibitor 1 是一种有效的，口服生物可利用的 ERK1/2 抑制剂，在 1 nM 时抑制 ERK1 达60％，抑制 ERK2 的 IC50 为 3.0 nM。
货号:ajcx39720
CAS:2095719-90-5
分子式:C29H32ClN5O4
分子量：550.05
溶解度:DMSO : 250 mg/mL (454.50 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively[1].

ERK1/2 inhibitor 1 (Compound 27) shows excellent antiproliferative potency with IC50s of 4.9 and 7.5 nM in A375 and Colo205 cells, respectively[1].

[1]. Heightman TD, et al. Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2. J Med Chem. 2018 Jun 14;61(11):4978-4992.

Protocol:

ERK2 3.0nM(IC50)

ERK1