| 应用 |
A Bcr-Abl (Bcr and c-Abl fusion), FGFR, and Flk-1 inhibitor |
| 产品介绍 |
Ponatinib (AP24534)是一种新型有效的作用于Abl， PDGFRα， VEGFR2， FGFR1和Src的多靶点抑制剂， IC50分别为0.37 nM， 1.1 nM， 1.5 nM， 2.2 nM和5.4 nM。 |
| 备注 |
Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM, respectively. |
| 生化机理 |
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. |
| 别名 |
AP 24534; AP-24534;3-(2-咪唑并[1,2-b]哒嗪-3-乙炔基)-4-甲基-N-[4-[(4-甲基-1-哌嗪基)甲基]-3-(三氟甲基)苯基]苯甲酰胺;AP 24534; AP24534; AP-24534;3-(2-Imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]benzamide |
