产品
编 号:F160485
分子式:C20H22F3N7OS
分子量:465.5
产品类型
结构图
CAS No: 1428569-85-0
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产品详情
生物活性:
GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma.
体内研究:
GDC-0339 (1-300 mg/kg; p.o; daily; for 21 days) is efficacious in RPMI8226 and MM.1S human multiple myeloma xenograft mouse models.GDC-0339 has a half-life of t1/2=0.9 h.Animal Model:Female C.B-17 SCID mice, RPMI8226 human multiple myeloma xenograft mouse model
Dosage:1mg/kg, 10 mg/kg, 50 mg/kg, 100 mg/kg, 200 mg/kg, 300 mg/kg
Administration:Oral administration; once daily; for 21 days
Result:Showed dose-dependent tumor growth inhibition.
体外研究:
GDC-0339 is cytostatic, with an IC50 of 0.1 μM for MM.1S cells.GDC-0339 treatment reveals a constellation of Pim downstream signaling events consistent with inhibition of Pim kinases.