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Afatinib Dimaleate

产品编号 T1773 CAS 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。

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Afatinib Dimaleate, CAS 850140-73-7

规格	价格/CNY	货期
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 * 10 mM (in DMSO)	￥ 633	现货

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其他形式的 Afatinib Dimaleate:

(S)-Afatinib
现货
Afatinib
现货
Afatinib D6
询价
Afatinib oxalate
询价
(R)-Afatinib
询价

选择批次

纯度: 100%

纯度: 99.66%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

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
分子量	718.08
分子式	C32H33ClFN5O11
CAS No.	850140-73-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (129.5 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.3926 mL	6.963 mL	13.926 mL	34.8151 mL
	5 mM	0.2785 mL	1.3926 mL	2.7852 mL	6.963 mL
	10 mM	0.1393 mL	0.6963 mL	1.3926 mL	3.4815 mL
	20 mM	0.0696 mL	0.3482 mL	0.6963 mL	1.7408 mL
	50 mM	0.0279 mL	0.1393 mL	0.2785 mL	0.6963 mL
	100 mM	0.0139 mL	0.0696 mL	0.1393 mL	0.3482 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

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. D Li, et al. Oncogene. 2008, 27(34):4702-4711. 2. Wang XK, et al. Cancer Res. 2014, 74(16):4431-4445. 3. Gurtner K, et al. Radiat Oncol. 2014, 9:261. 4. Schwab CL, et al. Br J Cancer. 2014, 111(9):1750-1756. 5. Janjiqian YY, et al. J Nucl Med. 2013, 54(6):936-943. 6. Li C, Sun Y D, Yu G Y, et al. Integrated Omics of Metastatic Colorectal Cancer[J]. Cancer Cell. 2020, 38(5): 734-747. e9

文献引用

1. Li C, Sun Y D, Yu G Y, et al. Integrated Omics of Metastatic Colorectal Cancer. Cancer Cell. 2020, 38(5): 734-747. e9 2. Mizuma K, Takashima A, Cubitt B, et al. The Pan-ErbB tyrosine kinase inhibitor afatinib inhibits multiple steps of the mammarenavirus life cycle. Virology. 2022

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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：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 μL，一共给药动物10 只，您使用的配方为5% 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 μL DMSO (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：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：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

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Afatinib Dimaleate 850140-73-7 Angiogenesis Autophagy JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR HER HKESC-1 NIH-3T3 cells ESCC orally active BIBW 2992 Apoptosis inhibit Epidermal growth factor receptor SLMT-1 BIBW-2992 c-Met/HGFR PKB 马来酸阿法替尼双马来酸盐阿法替尼 A431 BIBW2992 Akt NSCLC Afatinib anticancer Protein kinase B ErbB-1 p38 MAPK H3255 lung cancer HER2 Inhibitor H1666 BIBW 2992MA2 NCI-H1975 HKESC-2 Afatinib (BIBW2992) HER1 EC-1 Afatinib (BIBW2992) Dimaleate inhibitor

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Afatinib Dimaleate

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords