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Afatinib

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Chemical Structure| 850140-72-6 同义名 : BIBW 2992
CAS号 : 850140-72-6
货号 : A149039
分子式 : C24H25ClFN5O3
纯度 : 99%
分子量 : 485.938
MDL号 : MFCD12407405
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(216.08 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
动物实验配方：

2% DMSO+30% PEG 300+5% Tween 80+water 10 mg/mL

生物活性
靶点

  • EGFR/ErbB1

    EGFR (L858R), IC50:10 nM

    EGFR (wt), IC50:0.5 nM

  • HER2/ErbB2

    HER2, IC50:14 nM

  • ErbB4

    ErbB4, IC50:1 nM

  • HER2

    HER2, IC50:14 nM
描述 Afatinib E-isomer is an irreversible, dual EGFR/HER2 inhibitor, shows potent activity against wild-type and mutant forms of EGFR and HER2, with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.06mL

0.41mL

0.21mL

10.29mL

2.06mL

1.03mL

20.58mL

4.12mL

2.06mL
参考文献

[1]Wong CH, Ma BB, et al. Preclinical evaluation of afatinib (BIBW2992) in esophageal squamous cell carcinoma (ESCC). Am J Cancer Res. 2015 Nov 15;5(12):3588-99.

[2]Li D, Ambrogio L, et al. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene. 2008 Aug 7;27(34):4702-11.