产品
编 号:F753718
分子式:C30H38N6O2
分子量:514.66
产品类型
结构图
CAS No: 2561413-77-0
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产品详情
生物活性:
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 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.
体内研究:
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.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.
体外研究:
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.