ENMD-2076

产品说明书

Print
Chemical Structure| 934353-76-1 同义名 : -
CAS号 : 934353-76-1
货号 : A283012
分子式 : C21H25N7
纯度 : 98%
分子量 : 375.47
MDL号 : MFCD16619371
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 :

DMSO: 30 mg/mL(79.9 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • Aurora A

    Aurora A, IC50:14 nM

  • Aurora B

    Aurora B, IC50:350 nM

  • VEGFR3

    VEGFR3/FLT4, IC50:15.9 nM

  • VEGFR2

    VEGFR2/KDR, IC50:58.2 nM
描述 ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.32mL

2.66mL

1.33mL

26.63mL

5.33mL

2.66mL
参考文献

[1]Fletcher GC, Brokx RD, et al. ENMD-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative mechanisms of action. Mol Cancer Ther. 2011 Jan;10(1):126-37.

[2]Wang X, Sinn AL, et al. Preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor, ENMD-2076, against multiple myeloma. Br J Haematol. 2010 Aug;150(3):313-25.