JH-VIII-157-02 是一种 ALK 抑制剂，可抑制棘皮动物微管相关蛋白样 4-ALK (EML4-ALK)，对EML4-ALK G1202R、EML4-ALKwt、EML4-ALK C1156Y、EML4-ALK F1174L 和 EML4-ALK F1174L 的 IC50 均为 2 nM。

JH-VIII-157-02 is an inhibitor of ALK and inhibits echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) with IC50s of 2 nM for EML4-ALK G1202R, EML4-ALKwt, EML4-ALK C1156Y, EML4-ALK F1174L, and EML4-ALK F1174L.

JH-VIII-157-02 potently inhibits EML4-ALKS1206Y, EML4-ALKG1269A, EML4-ALKL1196M, EML4-ALK1151Tins, and EML4-ALKL1152R with IC50s of 2, 3, 58, 107 and 196 nM, respectively. JH-VIII-157-02 has selectivity at other kinases, including IRAK1, CLK4, RET, RET V804L, RET V804M and IRAK 4 with IC50s of 14 nM, 14 nM, 3 nM, 13 nM, 12 nM, and 465 nM, respectively[1].

In mice, JH-VIII-157-02 (10 mg/kg) exhibits good oral bioavailability and penetrates the central nervous system[1].

1639422-97-1

C28H27N5O2

465.55

DMSO:25 mg/mL (53.70 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years