主页 / 药理学 / Enzyme-Linked Receptors / Receptor Tyrosine Kinases (RTKs) / EGFR / EGFR Inhibitors / Afatinib dimaleate

Afatinib dimaleate

Cat. No. 6812 1 次引用 1 条评论 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
Pricing Availability   Qty
说明： Potent dual specificity EGFR/HER2 inhibitor; active in vivo
别名： BIBW2992
化学名： (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide dimaleate
纯度： ≥98% (HPLC)
说明书
引用文献 (1)
评论 (1)
文献 (1)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for Afatinib dimaleate

Afatinib dimaleate is a potent dual specificity EGFR/HER2 inhibitor (IC50 are 0.4, 0.5, 10, 14, 1 nM for EGFRL858R, EGFRwt, EGFR L858R/T790M, ErbB2 (HER2) and ErbB4 (HER4), respectively). 100-fold more active than Gefitinib in L858R-T790M EGFR double mutant cell line. Irreversibly binds EGFR and HER2. Suppresses the kinase activity of wild-type and activated EGFR and HER2 mutants, including erlotinib-resistant isoforms. Induces tumor regression in xenograft and transgenic lung cancer models.

化合物库 for Afatinib dimaleate

Afatinib dimaleate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。

技术数据 for Afatinib dimaleate

分子量 718.08
公式 C24H25ClFN5O3.2C4H4O4
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 850140-73-7
PubChem ID 15606394
InChI Key USNRYVNRPYXCSP-JUGPPOIOSA-N
Smiles CN(C/C=C/C(NC1=CC2=C(N=CN=C2NC3=CC(Cl)=C(C=C3)F)C=C1O[C@H]4CCOC4)=O)C.OC(/C=C\C(O)=O)=O.OC(/C=C\C(O)=O)=O

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Afatinib dimaleate

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
water 14.36 20 温和加热
DMSO 35.9 50

制备储备液 for Afatinib dimaleate

以下数据基于产品分子量 718.08。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
0.5 mM 2.79 mL 13.93 mL 27.85 mL
2.5 mM 0.56 mL 2.79 mL 5.57 mL
5 mM 0.28 mL 1.39 mL 2.79 mL
25 mM 0.06 mL 0.28 mL 0.56 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

产品说明书 for Afatinib dimaleate

分析证书/产品说明书
化学品安全技术说明书

参考文献 for Afatinib dimaleate

参考文献是支持产品生物活性的出版物。

Li et al (2008) BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene 27 4702 PMID: 18408761

If you know of a relevant reference for Afatinib dimaleate, please let us know.

按标靶查看相关产品

按产品操作查看相关产品

查看全部 EGFR Inhibitors

关键词: Afatinib dimaleate, Afatinib dimaleate supplier, BIBW2992, dual, specificity, EGFR, HER2, inhibitors, inhibits, potent, 6812, Tocris Bioscience

1 篇 Afatinib dimaleate 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Afatinib dimaleate 的部分引用包括：

Jürgen et al (2022) Intranasal delivery of a small-molecule ErbB inhibitor promotes recovery from acute and late-stage CNS inflammation. JCI Insight 7 PMID: 35393953

您是否知道使用了 Tocris Afatinib dimaleate 的优秀论文？ 请告知我们.

Afatinib dimaleate 的评论

平均评分: 5 (Based on 1 Review.)

5 星
100%
4 星
0%
3 星
0%
2 星
0%
1 星
0%

Have you used Afatinib dimaleate?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Filter by:


Easy to use!.
By Anonymous on 09/17/2022
分析类型： In Vitro
种属： Mouse
细胞系/组织： B16F0

I treated the mouse cell line with Afatinib, and detected the downstream EGFR tyrosine kinase activity by Western blot. The results were quantified and normalized to the vehicle-treated group.

review image

该领域的文献

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。

Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.