AV-412 free base

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Chemical Structure| 451492-95-8 同义名 : -
CAS号 : 451492-95-8
货号 : A116496
分子式 : C27H28ClFN6O
纯度 : 98+%
分子量 : 507.0
MDL号 : MFCD16038939
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(98.62 mM)，配合低频超声助溶，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

  • EGFR/ErbB1

    EGFR, IC50:0.75 nM

  • HER2/ErbB2

    ErbB2, IC50:19 nM

  • mutant EGFR

    EGFRL858R/T790M, IC50:0.51 nM

    EGFRT790M, IC50:0.79 nM
描述 AV-412 is a potent dual inhibitor of EGFR and ErbB2 (IC50=19 nM) tyrosine kinases, including the mutant EGFR (L858R IC50=0.51 nM, T790M IC50=0.79 nM). It inhibits autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.86mL

1.97mL

0.99mL

19.72mL

3.94mL

1.97mL
参考文献

[1]Suzuki T, Fujii A, et al. Ubiquitination and downregulation of ErbB2 and estrogen receptor-alpha by kinase inhibitor MP-412 in human breast cancer cells. J Cell Biochem. 2011 Sep;112(9):2279-86.

[2]Suzuki T, Fujii A, et al. Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptor and ErbB2 tyrosine kinase inhibitor. Cancer Sci. 2007 Dec;98(12):1977-84.