SGX-523

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更新时间： 2024-09-20 17:48:22

CAS号：1022150-57-7

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

价格：
￥需询单/1kg ￥需询单/1g ￥需询单/1mg

纯度： 98.0%

备货期： 需询单

库存： 询单

其他详情（用途，包装）：
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

供应商信息：

公司名：上海楼岚生物科技有限公司

认证状态： 未认证供应商

商品数： 2474件

电话： 52996696

地址： 沪南路2729弄1310号

地区： 上海市浦东新区

联系人： 孙先生

联系人电话： 021-52996696

邮件：sales@lollanechem.com

网址：http://www.bioll.com

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其他供应商价格：

2024-07-15 价格：需询单 SGX-523

2022-11-29 价格：￥需询单 SGX-523

2020-12-08 价格：￥1140.0 SGX-523

2022-02-19 价格：￥370.9 SGX-523

2017-11-14 价格：￥需询单 SGX-523

2021-05-10 价格：￥需询单 SGX-523

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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]喹啉价格

SGX-523

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