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Submit ReviewDacomitinib
说明： Potent irreversible pan ErbB inhibitor
别名： PF00299804
化学名： (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-2-butenamide
纯度： ≥98% (HPLC)
生物活性 for Dacomitinib
Dacomitinib is a potent irreversible pan ErbB inhibitor (IC50 values are 6.0, 45.7 and 73.7 nM for EGFR, ERBB2 and ERBB4, respectively). Inhibits mutant and wild type forms of ErbB, including EGFR T780M, and shows activity in NSCLC cell lines sensitive and resistant to Iressa (Cat. No. 3000). Inhibits tumor growth. Orally bioavailable.
许可信息
Sold for research purposes under agreement from Pfizer Inc.
化合物库 for Dacomitinib
Dacomitinib 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 Dacomitinib
| 分子量 | 469.94 |
| 公式 | C24H25ClFN5O2 |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1110813-31-4 |
| PubChem ID | 11511120 |
| InChI Key | LVXJQMNHJWSHET-AATRIKPKSA-N |
| Smiles | O=C(/C=C/CN1CCCCC1)NC2=C(OC)C=C(N=CN=C3NC4=CC=C(F)C(Cl)=C4)C3=C2 |
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 Dacomitinib
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| 1eq. HCl | 46.99 | 100 | |
| DMSO | 46.99 | 100 |
制备储备液 for Dacomitinib
以下数据基于产品分子量 469.94。 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.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.13 mL | 10.64 mL | 21.28 mL |
| 5 mM | 0.43 mL | 2.13 mL | 4.26 mL |
| 10 mM | 0.21 mL | 1.06 mL | 2.13 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
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产品说明书 for Dacomitinib
参考文献 for Dacomitinib
参考文献是支持产品生物活性的出版物。
Engelman et al (2007) PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefi. Cancer.Res. 67 11924 PMID: 18089823
Gonzales et al (2008) Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor. Mol.Cancer.Ther. 7 1880 PMID: 18606718
Li et al (2017) A ROR1-HER3-lncRNA signalling axis modulates the Hippo-YAP pathway to regulate bone metastasis. Nat.Cell.Biol. 19 106 PMID: 28114269
If you know of a relevant reference for Dacomitinib, please let us know.
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关键词: Dacomitinib, Dacomitinib supplier, Dacomitinib, ErbB, inhibitors, inhibits, EGFR, ERBB2, ERBB4, potent, irreversible, pan-ErbB, cancer, orally, bioavailable, PF00299804, 6231, Tocris Bioscience
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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!
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Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.