化学名称 : 1-环戊基-3-(1H-吡咯并[2,3-b]吡啶-5-基)-1H-吡唑并[3,4-d]嘧啶-4-胺
CAS : 1092788-83-4
英文名称: pp121/pp-121
英文同义词: PP121
溶解度:DMSO
储存条件:at -20 2 year
生物活性
MP470 is a multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Met, c-Kit, PDGFRalpha, Flt3, and c-Ret and with an IC50 of median 5 μM.MP470 reduced c-Met phosphorylation and enhanced radiation-induced cell kill by 0.4 logs in SF767 cells. Cells pretreated with MP470 had more ds DNA damage than cells treated with radiation alone. Mechanistically, MP470 was shown to inhibit dsDNA break repair and increase apoptosis. [1][2] In a study, the cytotoxicity of MP470 was evaluated on prostate cancer cell lines (LNCaP, PC-3 and DU-145). The drug was effective on LNCaP and PC-3 cells with an IC50 of ~4 μM and 8 μM, respectively. [3]
参考文献
[1] Welsh JW et al. Radiat Oncol. 2009 Dec 22;4:69.
[2] Qi W et al. BMC Cancer. 2009 May 11;9:142.