产品
编 号:F496052
分子式:C18H14ClFN4O
分子量:356.78
产品类型
结构图
CAS No: 882531-87-5
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产品详情
生物活性:
R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kd values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50 of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence.
体内研究:
R1530 (1.56, 25, and 50 mg/kg; p.o.; daily, for 28 days.) has notable antitumor activity across a broad range of human xenograft models, with minimal toxicity.Animal Model:Human tumor xenograft models
Dosage:1.56, 25 and 50 mg/kg
Administration:Oral administration; daily, for 28 days.
Result:Inhibited tumor growth in all models, with regression observed in all models tested at a 50 mg/kg dose.
体外研究:
R1530 exhibits potent in vitro antiproliferative activity in all of the tumor cell lines ( IC50 = 0.2?3.4 μM). R1530 inhibits the kinase activities of vascular endothelial growth factor receptor 2 (VGFr2), FGFr1 and PDGFr-β. R1530 has inhibition of VEGF and bFGF induces HUVEC proliferation ( IC50 = 49 and 118 nM).