TC ASK 10 是选择性的，口服有效的细胞凋亡信号调节激酶 1 抑制剂，IC50为 14 nM。它对其他代表性激酶的抑制活性低于 50％，除ASK2之外 (IC50为 0.51 μM)。

TC ASK 10 is a potent, selective and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1,IC50 = 14 nM). The IC50 value for ASK2 is 0.51 μM.

Streptozotocin (STZ)-induced JNK in INS-1 pancreatic β cells from 0.3 μM inhibited by TC ASK 10 (0-10 μM; 1 hour; INS-1 cells). Phosphorylation of p38 is also inhibited in a dosedependent manner.

In rats, Pharmacokinetic profiles are tested. TC ASK 10 (rat cassette doing at 0.1 mg/kg, iv and 1 mg/kg, po.) has a good oral bioavailability. The Cmax, Tmax and AUCpo,0-8h are 285.1 ng/mL, 1.67 h and 275.4 ng.h/mL, respectively for TC ASK 10.

1005775-56-3

C21H23Cl2N5O

432.35

DMSO:100 mg/mL (231.29 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years