BMS-599626

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Chemical Structure| 714971-09-2 同义名 : AC480
CAS号 : 714971-09-2
货号 : A434248
分子式 : C27H27FN8O3
纯度 : 98%
分子量 : 530.55
MDL号 : MFCD10565678
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
生物活性
靶点

  • EGFR/ErbB1

    HER1, IC50:20 nM

  • HER2/ErbB2

    HER2, IC50:30 nM

  • ErbB4

    HER4, IC50:190 nM

  • HER2

    HER2, IC50:30 nM
描述 AC480 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.
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00093730 Unspecified Adult Solid Tumor,... 展开 >> Protocol Specific 收起 << Phase 1 Completed - United States, California ... 展开 >> Jonsson Comprehensive Cancer Center at UCLA Los Angeles, California, United States, 90095-1781 收起 <<
NCT00207012 HER2 or EGFR Expressing Advanc... 展开 >>ed Solid Malignancies 收起 << Phase 1 Completed - France ... 展开 >> Local Institution Villejuif Cedex, France Spain Local Institution Barcelona, Spain 收起 <<
NCT00095537 Cancer Metast... 展开 >>ases 收起 << Phase 1 Completed - United States, Arizona ... 展开 >> Local Institution Scottsdale, Arizona, United States Local Institution Tucson, Arizona, United States United States, California Local Institution Los Angeles, California, United States 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.88mL

0.38mL

0.19mL

9.42mL

1.88mL

0.94mL

18.85mL

3.77mL

1.88mL
参考文献

[1]Torres MA, Raju U, 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.

[2]Wong TW, Lee FY, 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.