BMS-599626
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更新时间: 2025-12-29 07:51:56
CAS号:873837-23-1
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纯度: 99.0%
备货期: 10天
库存: 现货
其他详情(用途,包装):
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:873837-23-1 常用中文名:[4-[[1-[(3-氟苯基)甲基]-1H-吲唑-5-基]氨基]-5-甲基吡咯并[2,1-f][1,2,4]三嗪-6-基]氨基甲酸 (3S)-3-吗啉基甲基酯盐酸盐 常用英文名:BMS-599626 (Hydrochloride) 分子式:C27H28ClFN8O3 分子量:567.014 密度:N/A 沸点:N/A 熔点:N/A 闪点:N/A 储存条件:-20°C,保存于惰性气体中
供应商信息:
公司名:上海念兴实业有限公司 推荐
认证状态: 已认证供应商
商品数: 403768件
电话: 18916513247
地址: 2222 Huancheng Road, Juyuan New District, Jiading District, Shanghai
地区: 上海市普陀区
联系人: 小陈
联系人电话: 0086-021-52280163
邮件:sales@echemcloud.com
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公司名:上海化源世纪贸易有限公司
区域:上海市普陀区
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联系人:徐经理
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2024-07-15 价格:需询单
2021-02-06 价格:¥5011.0
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BMS-599626价格为, 由BMS-599626生产厂家上海念兴实业有限公司提供,供应信息包括纯度,备货期/库存,供货能力等。>>电脑版:BMS-599626_价格_生产厂家【上海念兴实业有限公司】
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