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Afatinib Dimaleate

产品编号 T1773Cas号 850140-73-7
别名 马来酸阿法替尼, 双马来酸盐阿法替尼, BIBW2992, Afatinib, BIBW 2992MA2, Afatinib (BIBW2992) Dimaleate

Afatinib Dimaleate (BIBW 2992MA2) 是一种可口服的苯胺基-喹唑啉衍生物和受体酪氨酸激酶表皮生长因子受体家族的抑制剂,具有抗肿瘤活性。它抑制 EGFRwt、EGFRL858R、EGFRL858R/T790M 和 HER2的 IC50分别为0.5 nM、0.4 nM、10 nM 和 14 nM。

Afatinib Dimaleate

Afatinib Dimaleate

纯度: 99.66%
产品编号 T1773 别名 马来酸阿法替尼, 双马来酸盐阿法替尼, BIBW2992, Afatinib, BIBW 2992MA2, Afatinib (BIBW2992) DimaleateCas号 850140-73-7

Afatinib Dimaleate (BIBW 2992MA2) 是一种可口服的苯胺基-喹唑啉衍生物和受体酪氨酸激酶表皮生长因子受体家族的抑制剂,具有抗肿瘤活性。它抑制 EGFRwt、EGFRL858R、EGFRL858R/T790M 和 HER2的 IC50分别为0.5 nM、0.4 nM、10 nM 和 14 nM。

规格价格库存数量
1 mg¥ 176现货
5 mg¥ 357现货
10 mg¥ 576现货
25 mg¥ 715现货
50 mg¥ 867现货
100 mg¥ 1,230现货
200 mg¥ 1,730现货
500 mg¥ 2,990现货
1 g¥ 4,390现货
1 mL x 10 mM (in DMSO)¥ 633现货
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纯度:99.66%
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产品介绍

生物活性
产品描述
Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.
靶点活性
EGFR (WT):0.5 nM, EGFR (L858R):0.4 nM, EGFR (L858R/T790M):10 nM, HER2:14 nM
体外活性
在MDA-MB-453移植瘤模型中,口服给药 Afatinib(20 mg/kg),下调EGFR和AKT磷酸化水平,能够诱导肿瘤衰退.在HER2阳性胃癌NCI-N87移植瘤模型中,口服 Afatinib(25 mg/kg)能够消除肿瘤.在A7、A431、FaDu、UT-SCC-14和UT-SCC-15移植瘤模型中,口服给药 Afatinib(30 mg/kg)能够抑制肿瘤生长.
体内活性
在表达野生型(H1666)或L858R/T790M (NCI-H1975) EGFR的肺癌细胞系中,Afatinib能够更有效的抑制细胞生长。在表达HER2 776insV (NCI-H1781) 或EGFR E746_A750del (HCC827)的NSCLC细胞系中,Afatinib能够更抑制细胞生长。
激酶实验
In vitro kinase activity assay: EGFR kinase: Each 100 μL enzyme reaction contained 10 μL of inhibitor in 50% Me2SO, 20 μL of substrate solution (200 mM HEPES pH 7.4, 50 mM Mg-acetate, 2.5 mg/mL poly (EY), 5 μg/mL bio-pEY) and 20 μL enzyme preparation. The enzymatic reaction is started by addition of 50 μL of a 100 μM ATP solution made in 10 mM MgCl2. Assays are carried out at room temperature for 30 min and terminated by the addition of 50 μL of stop solution (250 mM EDTA in 20 mM HEPES pH 7.4). 100 μL are transferred to a streptavidin coated microtiterplate, after an incubation time of 60 min at room temperature the plate is washed with 200 μL of wash solution (50 mM Tris, 0.05% Tween20). A 100 μL aliquot of a HRPO- labeled anti-PY antibody (PY20H Anti-Ptyr:HRP ) 250 ng/mL are added to the wells. After 60 min of incubation, the plate is washed three times with a 200 μL wash solution. The samples are then developed with a 100μL TMB Peroxidase Solution (A:B= 1:1). The reaction is stopped after 10 min. The plate is transferred to an ELISA reader and extinction is measured at OD450 nM. HER2-IC enzyme: Enzyme activity is assayed in the presence or absence of serial inhibitor dilutions performed in 50 % Me2SO. Each 100 μL reaction contains similar components as described for EGFR kinase assay with addition of 1000 μM Na3VO4. The enzymatic reaction is started by addition of 50μL of 500 μM ATP solution made in 10 mM Mg-acetate. The dilution of the enzyme is set so that incorporation of phosphate into bio-pEY is linear with respect to time and amount of enzyme. The enzyme preparation is diluted in 20 mM HEPES pH 7.4, 130 mM NaCl, 0.05% Triton X-100, 1 mM DTT and 10% glycerol. Assays are carried out at room temperature for 30 min and terminated by the addition of 50 μL of stop solution. Src kinase assays: Each 100 μL reaction contained 10 μL of inhibitor in 50 % Me2SO, 20μL of enzyme preparation, 20 μL of substrate solution supplemented with 1000 μM Na3VO4.The enzymatic reaction is started by addition of 50 μL of a 1000 μM ATP solution made in 10 mM Mg-acetate. BIRK kinase assay: 250 mM Tris pH 7.4, 10 mM DTT, 2.5 mg/mL poly(EY), 5 mg/mL bio-pEY is used as substrate solution and enzymatic reaction is started by addition of 50 μL of a 2 mM ATP solution made in 8 mM MnCl2, 20 mM Mg-acetate. VEGF2 and HGFR kinase assays: Assays are carried out at room temperature for 20 minutes and terminated by the addition of 10 μL of 5 % H3PO4. The precipitate is then trapped onto GF/B filters using a 96 well filter mate universal harvester. After extensive washing the filter plate is dried for 1 h at 50°C, sealed and incorporated radioactivity is determined by scintillation counting using a TopCount? or a Microbeta b counter?.
细胞实验
Cytotoxicity is determined using MTT assay. The IC 50 value is de?ned as the drug concentration resulting in 50% cell death. Both the ?tted sigmoidal dose response curve and IC50 are calculated by Bliss method.(Only for Reference)
别名马来酸阿法替尼, 双马来酸盐阿法替尼, BIBW2992, Afatinib, BIBW 2992MA2, Afatinib (BIBW2992) Dimaleate
化学信息
分子量718.08
分子式C32H33ClFN5O11
CAS No.850140-73-7
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 50 mg/mL (69.63 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM1.3926 mL6.9630 mL13.9260 mL69.6301 mL
5 mM0.2785 mL1.3926 mL2.7852 mL13.9260 mL
10 mM0.1393 mL0.6963 mL1.3926 mL6.9630 mL
20 mM0.0696 mL0.3482 mL0.6963 mL3.4815 mL
50 mM0.0279 mL0.1393 mL0.2785 mL1.3926 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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