| 应用 |
A c-Abl, PDGFR, and c-kit inhibitor |
| 产品介绍 |
Imatinib Mesylate (STI571)是Imatinib的甲磺酸盐，具有较好的口服生物利用度，是一种多靶点的抑制剂，同时作用于v-Abl， c-Kit和PDGFR，IC50分别为0.6 μM， 0.1 μM 和0.1 μM。 |
| 备注 |
Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively. |
| 生化机理 |
Imatinib mesylate is a small molecule that inhibits the c-Abl protein-tyrosine kinase, a kinase specifically important for proliferation of chronic myelogenous leukemia (CML). A translocation event between chromosomes 9 and 22 generates the Philadelphia chromosome, which then produces the Bcr-Abl fusion protein with aberrant kinase activity that promotes rapid cell proliferation. Imatinib binds up this crucial kinase, halting CML related growth. Imatinib mesylate has further been displayed to inhibit PDGFR and tyrosine kinases associated with c-Kit. |
| 别名 |
甲磺酸伊马替尼;伊马替尼甲磺酸盐;4-[(4-甲基-1-哌嗪基)甲基]-N-[4-甲基-3-[4-(3-吡啶基)-2-嘧啶基]氨基]-苯基]苯甲酰胺甲磺酸盐;CGP 57148;Genfatinib;Glivec;STI-571;Imatinib methanesulfonate;4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-phenyl]benzamide methanesulfonate;4-[(4-Methylpiperazin-1-yl)methyl]-N-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)benzamide mesylate |
