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BMS-599626

MCE 国际站：BMS-599626

品牌：MedChemExpress (MCE)

货号：HY-10251

CAS 号：714971-09-2

生物活性： BMS-599626 (AC480) 是一种选择性强、口服生物利用度高的 HER1 和 HER2 抑制剂，其 IC50 值分别为 20 nM 和 30 nM。BMS-599626 对 HER4 的抑制效力约为 HER1 和 HER2 的 1/8（IC50=190 nM），而对 VEGFR2、c-Kit、Lck 和 MEK 的抑制效力则高出 100 倍以上。BMS-599626 可抑制肿瘤细胞增殖，并有可能增强肿瘤对放射治疗的反应[1][2]。

体外研究(In Vitro)：BMS-599626 inhibits the proliferation of tumor cells that are dependent on HER1/HER2 signaling. BMS-599626 (0.03-8 µM; 1 huors) results in the inhibition of receptor autophosphorylation, as well as MAPK phosphorylation, with IC50s of 0.3 and 0.22 µM, respectively, in Sal2 cells which express a CD8HER2 fusion protein[1]. BMS-599626 abrogates 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 µM.In GEO cells, HER1 phosphorylation is stimulated by treatment with EGF and is inhibited by BMS-599626 (IC50=0. 75 µM).There is also nearly complete inhibition of EGF-dependent MAPK (0. 8 µM) but only partial inhibition of AKT signaling.The latter likely reflects the activation of AKT by multiple upstream signals.Treatment of N87 cells with BMS-599626 leads to the inhibition of HER2 (0. 38 µM), which is expressed to a high level because of gene amplification, as well as MAPK and AKT phosphorylation (0.35 µM for both)[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]. MCE尚未独立确认这些方法的准确性。 仅供参考。

体内研究(In Vivo)：BMS-599626 (60-240 mg/kg; p.o.; daily for 14 days) results in a dose-dependent inhibition of Sal2 tumor growth[1]. BMS599626 treatment results in the inhibition of GEO xenograft tumor growth when given once daily for 14 days. In addition to efficacy in the Sal2, GEO, and KPL4 models, BMS-599626 has similar antitumor activity in other HER2 amplified xenograft models including the BT474 breast and N87 gastric tumors, as well as other HER1-overexpressing non-small-cell lung tumors (A549 and L2987)[1]. BMS599626 given before and during irradiation improved the radioresponse of HN5 tumors in vivo[2]. MCE尚未独立确认这些方法的准确性。 仅供参考。

分子量：530.55

Formula：C27H27FN8O3

性状：固体

颜色：White to off-white

运输条件：美国大陆地区的室温；其他地区可能有所不同。

储存方式：粉末 -20°C 3年

文献引用：MCE 顾客使用本产品发表 3 篇科研文献

提供质量检测报告：Data Sheet、SDS、COA、HNMR、RP-HPLC、NP-HPLC、LCMS、产品使用指南

产品活性：BMS-599626 (AC480) 是一种选择性的口服生物利用度 HER1 和 HER2 抑制剂，其 IC50 分别为 20 和 30 nM。BMS-599626 对 HER4 的 IC50 值为 190 nM，对 VEGFR2、c-Kit、Lck、MEK 的抑制强度降低了100倍。BMS-599626抑制肿瘤细胞增殖，并有可能增加肿瘤对放疗的反应。

相关产品：Bemcentinib | Bemcentinib (Standard) | Dimethyl sulfoxide (GMP Like) | Dimethyl sulfoxide, meets analytical specification of Ch.P. | Dimethyl sulfoxide (Standard) | Ripretinib | Bemcentinib (GMP) | Imiquimod | Dimethyl sulfoxide | Dimethyl sulfoxide, cryoprotectant vitrification agent | TX1-85-1 | RAF265

热门产品线：抑制剂 | 稳定性同位素标记物 | 脂质 | 糖类

Trending products：Inhibitors | Isotope-Labeled Compounds | Lipids | Saccharides

参考文献：
[1]. Wong TW, et al. Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin Cancer Res. 2006 Oct 15;12(20 Pt 1):6186-93.
[2]. Torres MA, et al. AC480, formerly BMS-599626, a pan Her inhibitor, enhances radiosensitivity and radioresponse of head and neck squamous cell carcinoma cells in vitro and in vivo. Invest New Drugs. 2011 Aug;29(4):554-61.