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BMS-599626 BMS599626

更新时间:2025-08-19 12:46:26 采购访问:38次

常用名 [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 CAS号 873837-23-1
价格 $需询单/100g $需询单/1kg $需询单/100kg $需询单/1000kg 纯度 98.0%
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 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: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

达阳化工(杭州)有限公司 认证供应商

认证状态:已认证供应商
商品数:50181件
电话:+86571-88938639
地址:浙江省杭州市西湖区文三路259号2栋9楼
地区: 浙江省 杭州市 西湖区
联系人:王小姐
联系人电话:+86-571-8893-8639
邮件:enquiry@dycnchem.com
网址:http://www.dycnchem.com
主要市场:Mainly in Southeast Asia and European and American markets
年贸易额:10 to 20 million USD
外贸占销售比例:90%
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