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AC480(BMS-599626)

更新时间:2025-09-12 13:17:55 采购访问:17次

常用名 BMS-599626 CAS号 714971-09-2
价格 纯度 98.0%
备货期 10天 库存 现货
 产品详情(用途,包装等)
用途:
AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc.IC50 value: 20 nM (HER1); 30 nM (HER2) [1]Target: HER1/HER2in vitro: BMS-599626 inhibited HER1 and HER2 with IC50 of 20 and 30 nmol/L, respectively, and was highly selective when tested against a broad panel of diverse protein kinases. Biochemical studies suggested that BMS-599626 inhibited HER1 and HER2 through distinct mechanisms. BMS-599626 abrogated HER1 and HER2 signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC50 in the range of 0.24 to 1 micromol/L. BMS-599626 was highly selective for tumor cells that depend on HER1/HER2 and had no effect on the proliferation of cell lines that do not express these receptors. In tumor cells that are capable of forming HER1/HER2 heterodimers, BMS-599626 inhibited heterodimerization and downstream signaling [1]. At the molecular level, in HN-5 cells the agent inhibited the expression of pEGFR, pHER2, cyclins D and E, pRb, pAkt, pMAPK, pCDK1 and 2, CDK 6, and Ku70 proteins. The drug also induced accumulation of cells in the G1 cell cycle phase, inhibited cell growth, enhanced radiosensitivity, and prolonged the presence of γ-H AX foci up to 24 h after radiation [2].in vivo: BMS-599626 had antitumor activity in models that overexpress HER1 (GEO), as well as in models that have HER2 gene amplification (KPL4) or overexpression (Sal2), and there was good correlation between the inhibition of receptor signaling and antitumor activity [1]. The drug given before and during irradiation improved the radioresponse of HN5 tumors in vivo [2].
物理化学性质:
CAS号:714971-09-2
常用中文名:BMS-599626
常用英文名:AC480 (BMS-599626)
分子式:C27H27FN8O3
分子量:530.554
密度:1.5±0.1 g/cm3
沸点:N/A
熔点:N/A
闪点:N/A
储存条件:<0°C;避免加热

供应商信息

上海化源世纪贸易有限公司 认证供应商

认证状态:已认证供应商
商品数:396716件
电话:53555033
地址:上海市普陀区金沙江路1759号圣诺亚大厦B座
地区: 上海市 上海市 普陀区
联系人:徐经理
联系人电话:13311869306
邮件:xuqm@chemsrc.com
网址:http://www.chemsrc.com
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参考价格:¥1754/10mg
其他供应商价格:
2022-02-19 AC480 (BMS-599626)
价格:¥851.9
2023-09-20 BMS599626
价格:¥需询单
2018-02-11 AC480 (BMS-599626)base
价格:¥需询单
2021-02-06 AC480 (BMS-599626)
价格:¥2989.0

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