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1.7nM和5.3nM。可透过血脑屏障。
货号:ajcx31666
CAS:N/A
分子式:C30H38N6O2
分子量：514.66
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

WF-47-JS03 is a potent and selective RET kinase inhibitor with IC50s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells, 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 IC50s 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

[1]. Casey J N Mathison , et al. Efficacy and Tolerability of Pyrazolo[1,5- a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma. ACS Med Chem Lett. 2020 Feb 12;11(4):558-565.