Ensartinib hydrochloride 是双重的 ALK/MET 抑制剂，IC50分别<0.4 nM 和 0.74 nM。

Ensartinib dihydrochloride is a potent new-generation ALK inhibitor with high activity against CNS metastases and a broad range of known crizotinib-resistant ALK mutations. It potently inhibits both wild-type ALK and ALK variants (C1156Y, F1174, G1202R, L1196M, S1206R, and T1151 mutants) with in vitro IC50s of<4 nM.

Ensartinib potently inhibits both wild-type ALK and all evaluated ALK variants (C1156Y, F1174, G1202R, L1196M, S1206R, and T1151 mutants) with in vitro IC50s of<4 nM. Besides ALK, ensartinib also potently inhibits GOPC-ROS1, TPM3-TRKA, and TRKC with an IC50 of<1 nM, and inhibits EphA1, EphA2, EphB1 and c-MET with an IC50 of 1-10 nM[1].

2137030-98-7

C26H29Cl4FN6O3

634.36

X-396 dihydrochloride;Ensartinib dihydrochloride

DMSO:33mg/ml (52.02 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years