性狀: | 屬性溶解性Soluble in DMSO (100 mM), ethanol (50 mM), methanol, and water (<1 mg/ml) at 25 °C.存貯條件儲存溫度-20°C熔點>160 °C描述產(chǎn)品介紹Ponatinib (AP24534)是一種新型有效的作用于Abl, PDGFRα, VEGFR2, FGFR1和Src的多靶點抑制劑, IC50分別為0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM和5.4 nM。用途A Bcr-Abl (Bcr and c-Abl fusion), FGFR, and Flk-1 inhibitor生化機理AP 24534 is a small molecule, multi-target kinase inhibitor known to potently inhibit Bcr-Abl (the fusion protein of Bcr and c-Abl), Flk-1(VEGFR2) and FGFR. It also exhibits inhibitory activity against PDGFRα, c-Src and c-Kit. AP 24534 inhibits the proliferation of mutant FLT3-positive cells (IC50 of 13 nM), which inhibits mutant FLT3 phosphorylation (IC50 of 1 nM) and the proliferation of Bcr-Abl1 T315I-positive Ba/F3 cells with an IC50 of 8 nM.包裝P127550-10mg,P127550-50mg,P127550-250mg in glass bottle |
用途: | AP24534 is a novel potent, orally available small molecule multitargeted kinase inhibitor with IC50 of 0.37, 2, 1.5, 2.2, 1.1, 1and 0.24 nM for native pan-BCR-ABL, mutated form, VEGFR2, FGFR1, PDGFRα, mutant FLT3 phosphorylation and LYN. [1] O’Hare T et al. Cancer Cell. 2009 Nov 6;16(5):401-12. |