WF-47-JS03 是一种有效的选择性RET激酶抑制剂，比对激酶插入域受体 (KDR) 的选择性高 500 多倍。WF-47-JS03 作用于转染 KIF5B-RET 的 Ba/F3 细胞和转染 CCDC6-RET 的 LC-2/ad 肺癌细胞，IC50分别为 1.7 nM 和 5.3 nM。可透过血脑屏障。

WF-47-JS03 is a potent and selective RET kinase inhibitor with IC 50 s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells and CCDC6-RET transfected LC-2/ad lung cancer cells, respectively. WF-47-JS03 demonstrates >500-fold selectivity against kinase insert domain receptor (KDR). Effective brain penetration [1].

WF-47-JS03 inhibits Tel-KDR transfected Ba/F3 cells and Ba/F3 wild-type cell lines with IC 50 s of 0.99 and 1.5 μM, respectively [1].

WF-47-JS03 significantly inhibits tumor growth in RIE KIF5B-RET xenograft mice and is well tolerated at 1, 3, and 10 mg/kg in the 10 day study [1]. Animal Model: Female 6-8 week old Harlan Foxn1 nude mice with RIE-RET-KIF5B transgenic cell line Dosage: 1, 3, 10 mg/kg Administration: Dosed orally, 1x daily for 10 days Result: Inhibited tumor growth in RIE KIF5B-RET xenograft mice.

C30H38N6O2

514.66

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years