General description
一种选择性的AXL激酶抑制剂，IC50：14nM。
BGB324 is a selective small molecule inhibitor of Axl kinase, which showed activity to blocks tumor spread and prolongs survival in models of metastatic breast cancer. The receptor tyrosine kinase Axl may play an important role in cancer progression, invasion, metastasis, drug resistance, and patient mortality. R428 inhibits Axl with low nanomolar activity and blocked Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production。
BGB324是Axl激酶的选择性小分子抑制剂，在转移性乳腺癌模型中显示出阻断肿瘤扩散和延长生存期的活性。 受体酪氨酸激酶Axl可能在癌症进展，侵袭，转移，耐药性和患者死亡率中起重要作用。 R428抑制具有低纳摩尔活性的Axl，并阻断Axl依赖性事件，包括Akt磷酸化，乳腺癌细胞侵袭和促炎性细胞因子产生。
Properties
| Iupac Name： | 1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N~3~-[(7S)-7-(1-pyrrolidinyl)-6,7,8,9-tetrahydro-5H-benzo[a]cyclohepten-2-yl]-1H-1,2,4-triazole-3,5-diamine |
| Inchi Code | 1S/C30H34N8/c31-29-33-30(32-24-13-10-20-11-14-25(15-12-22(20)18-24)37-16-3-4-17-37)36-38(29)27-19-23-8-5-7-21-6-1-2-9-26(21)28(23)35-34-27/h1-2,6,9-10,13,18-19,25H,3-5,7-8,11-12,14-17H2,(H3,31,32,33,36)/t25-/m0/s1 |
| Inchi Key | KXMZDGSRSGHMMK-VWLOTQADSA-N |
安全信息
