甲磺酸氟马替尼
| CAS号 | 895519-91-2 | 货号 | BCP08647 |
| 中文名 | 甲磺酸氟马替尼 | ||
| 英文名 | Flumatinib mesylate | ||
| 中文别名 | |||
| 英文别名 | HHGV678 mesylate; HHGV 678 mesylate ; HHGV-678 mesylate; HH-GV-678 mesylate; | ||
| 分子式 | C30H33F3N8O4S | 分子量 | 658.69 |
| 生物活性 | Flumatinib Mesylate is the orally bioavailable, mesylate salt form of the tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity. Upon administration, flumatinib inhibits the wild-type forms of Bcr-Abl, platelet-derived growth factor receptor (PDGFR) and mast/stem cell growth factor receptor (SCFR; c-Kit) and forms of these proteins with certain point mutations. This results in the inhibition of both Bcr-Abl-, PDGFR- and c-Kit-mediated signal transduction pathways, and the proliferation of tumor cells in which these kinases are overexpressed. Bcr-Abl fusion protein is an abnormal, constitutively active enzyme expressed in Philadelphia chromosome positive chronic myeloid leukemia (CML), acute lymphoblastic leukemia (ALL) or acute myelogenous leukemia (AML). PDGFR, upregulated in many tumor cell types, is a receptor tyrosine kinase essential to cell migration and the development of the microvasculature. c-kit, a receptor tyrosine kinase mutated and constitutively activated in certain tumors, plays a key role in tumor cell survival, proliferation, and differentiation. | ||
| 信号通路 | Angiogenesis/Protein Tyrosine Kinase | ||
| 靶 点 | Src/Bcr Abl PDGFR c Kit | ||
结构式
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