| Bioactivity | 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[1][2]. | ||||||||||||
| Invitro | R1530 exhibits potent in vitro antiproliferative activity in all of the tumor cell lines ( IC50 = 0.2−3.4 μM)[1]. 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)[1]. | ||||||||||||
| Name | R1530 | ||||||||||||
| CAS | 882531-87-5 | ||||||||||||
| Formula | C18H14ClFN4O | ||||||||||||
| Molar Mass | 356.78 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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