ARS-853 是一种选择性共价KRas G12C抑制剂，IC50为 2.5 μM。它通过与 GDP 结合的癌蛋白结合并阻止激活来抑制突变 KRas 驱动的信号传导。

ARS-853 is an inhibitor of K-RASG12C(IC50 : 2.5 μM), a mutant form of K-RAS that accumulates in the active GTP-bound state in certain cancer cells

ARS-853 decreases phosphorylation of c-RAF, ERK, and Akt. ARS853 inhibits proliferation of six lung cancer cell lines containing the K-RASG12C mutation, including H358 cells (IC50 = 2.5 μM), but does not inhibit proliferation of PC-9 cells, which contain wild-type K-RAS[1].

1629268-00-3

C22H29ClN4O3

432.95

DMSO:71 mg/mL (164.00 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years