R1530

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

R1530 is a multikinase inhibitor with antineoplastic and antiangiogenesis activities.

R1530 is a multikinase inhibitor with antineoplastic and antiangiogenesis activities.(In Vitro):R1530 inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as VEGFR-1/2/3, PDGFR, Flt-3 and FGFR-1/2. R1530 enables polyploid cancer cells to undergo apoptosis or senescence, which translates into potent in vitro and in vivo efficacy. Normal proliferating cells are resistant to R1530-induced polyploidy. The mitotic checkpoint kinase BubR1 is downregulated during R1530-induced mitotic exit, possibly as a result of PLK4 inhibition. R1530 strongly inhibits human tumor cell proliferation. Growth factor-driven endothelial and fibroblast proliferation is also inhibited.(In Vivo):Showing significant tumor growth inhibition in a lung cancer xenograft model, R1530 was administered at doses ranging from once daily, weekly and twice weekly (3.125-50 mg/kg qd, 100 mg/kg qw, 100 mg/kg kg biw). Tumor regression occurred in all models treated with the maximum tolerated daily dose (50 mg/kg). Doses of 25 and 50 mg/kg qd resulted in biologically significant increases in survival in all models tested. After oral administration to nude mice, R1530 showed good tissue permeability. Exposure was dose-dependent, up to 100 mg/kg when administered orally.

R 1530; R-1530

Angiogenesis

VEGFR

VEGFR

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882531-87-5

356.8

C18H14ClFN4O

>98% (HPLC)

——

COc1cc2N=C3NNC(C)=C3N=C(c3ccccc3Cl)c2cc1F

——

(-20℃)

With Ice Pack

≥ 2 years