SGX-523
更新时间：2025-08-21 18:25:58
| 常用名 | 6-[[6-(1-甲基-1H-吡唑-4-基)-1,2,4-噻唑并[4,3-b]吡嗪-3-基]硫代]喹啉 | CAS号 | 1022150-57-7 |
|---|---|---|---|
| 价格 | ￥需询单/1mg | 纯度 | 98.0% |
| 备货期 | 3天 | 库存 | 现货 |
| 产品详情（用途，包装等）
用途： SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α.IC50 value: 4 nM [1]Target: Metin vitro: SGX-523 belongs to the class of c-Met/hepatocyte growth factor receptor (HGFR) tyrosine kinase inhibitors. SGX-523 stabilizes MET in a unique inactive conformation that is inaccessible to other protein kinases, suggesting an explanation for its selectivity. SGX523 potently inhibits the purified MET catalytic domain but not the closely related receptor tyrosine kinase RON. SGX523 indicates ATP-competitive inhibition with higher apparent affinity for the less active, unphosphorylated form of MET [MET-KD(0P), with a Ki of 2.7 nM] versus the more active phospho-enzyme [MET-KD(3P), with a Ki of 23 nM], a phenomenon consistent with preferential binding to an inactive enzyme conformation. SGX523 inhibits MET-mediated signaling, cell proliferation and cell migration at nanomolar concentrations but had no effect on signaling dependent on other protein kinases, including the closely related RON, even at micromolar concentrations [1].in vivo: SGX523 significantly retards the growth of preestablished GTL16 tumors when administered orally at doses of ≥10 mg/kg twice daily. SGX523 potently inhibits U87MG tumor growth; at 30 mg/kg dosed twice daily, SGX523 leads to clear regression of U87MG tumors. SGX523, dosed twice daily at 30 mg/kg, also retards the growth of H441 tumors with concomitant reduction in tumor MET autophosphorylation levels. SGX523 inhibition of MET in vivo is associated with the dose-dependent inhibition of growth of tumor xenografts derived from human glioblastoma, lung and gastric cancers, confirming the dependence of these tumors on MET catalytic activity [1]. 物理化学性质： CAS号：1022150-57-7 常用中文名：6-[[6-(1-甲基-1H-吡唑-4-基)-1,2,4-噻唑并[4,3-b]吡嗪-3-基]硫代]喹啉 常用英文名：SGX-523 分子式：C18H13N7S 分子量：359.408 密度：1.5±0.1 g/cm3 沸点：N/A 熔点：N/A 闪点：N/A 储存条件：-20°C |
- 上海化源生化科技有限公司
- 上海市 上海市 普陀区
- 产品名：SGX-523
- 价格：
- 纯度：98.0%
- 备货期：10天
- 联系人：徐经理
- 上海源溪生物科技有限公司
- 上海市 上海市 浦东新区
- 产品名：SGX-523
- 价格： ￥需询单/1g
- 纯度：98.9%
- 备货期：1天
- 联系人：赖经理
- 上海阿拉丁生化科技股份有限公司
- 上海市 上海市 浦东新区
- 产品名：SGX-523
- 价格： ￥370.9/10mg ￥1480.9/50mg ￥231.9/5mg ￥需询单/1g
- 纯度：98.0%
- 备货期：1天
- 联系人：阿拉丁
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6-[[6-(1-甲基-1H-吡唑-4-基)-1,2,4-噻唑并[4,3-b]吡嗪-3-基]硫代]喹啉生产厂家
参考价格：$95/10mM*1mLinDMSO