现货,ENMD-2076,CAS号: 1291074-87-7 ,美国进口,血管生成(Angiogenesis) ,Flt, Flt 抑制剂, ENMD-2076

信号转导通路: 血管生成(Angiogenesis) >> Flt >> Flt 抑制剂 >> ENMD-2076http://selleck.cn/enmd-2076-S1181.html

技术数据:

分子量(MW): 525.56

化学式:

C25H31N7O6

溶解度: DMSO ≥105mg/mL Water ≥1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1291074-87-7

生物活性

 

ENMD-2076 is a novel, orally bioavailable multitargeted antiangiogenic and Aurora kinase inhibitor with IC50 of 3, 13, 350, 23, 40, 93 and 120 nM for Flt-3, AurA, AurB, Src, KDR/VEGFR2 and FGFR1. ENMD-2076 is relatively selective for the Aurora A isoform in comparison to Aurora B. [1] ENMD-2076 has demonstrated significant, dose-dependent preclinical activity as a single agent, including tumor regression, in multiple xenograft models (e.g. breast, colon, leukemia), as well as activity towards ex vivo-treated human leukemia patient cells. ENMD-2076 is currently in Phase 1 clinical studies in solid tumors and multiple myeloma. ENMD-2076 demonstrated robust antitumor activity against cell line and patient-derived xenograft models of CRC that is detectable by functional imaging, supporting clinical investigation of this agent in human colorectal cancer. [1][2]

 

参考文献

Assessment of the In vivo Antitumor Effects of ENMD-2076, a Novel Multitargeted Kinase Inhibitor, against Primary and Cell Line-Derived Human Colorectal Cancer Xenograft Models Erica L. Bradshaw-Pierce, Natalie J. Serkova, et al. Clin Cancer Res 2010;16:2989-2998

ENMD-2076 Is an Orally Active Kinase Inhibitor with Antiangiogenic and Antiproliferative Mechanisms of Action Richard D. Brokx, Trisha A. Denny, et al. Mol Cancer Ther 2011;10:126-137

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