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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-Dacomitinib
Dacomitinib

Chemical Structure : Dacomitinib

CAS No.: 1110813-31-4

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Dacomitinib (PF-00299804, PF-299804)

货号: PC-43452Not For Human Use, Lab Use Only.

Dacomitinib (PF-00299804, PF-299804) is a potent, irreversible, orally active pan-ErbB receptor tyrosine kinase inhibitor with IC50 of 6, 45.7 and 73.7 for EGFR, ERBB2 and ERBB4, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Dacomitinib (PF-00299804, PF-299804) is a potent, irreversible, orally active pan-ErbB receptor tyrosine kinase inhibitor with IC50 of 6, 45.7 and 73.7 for EGFR, ERBB2 and ERBB4, respectively.
Dacomitinib (PF-00299804, PF-299804) irreversibly inhibits erbB tyrosine kinase activity through binding at the ATP site and covalent modification of nucleophilic cysteine residues in the catalytic domains of erbB family members inhibits erbB1 autophosphorylation in the A431 human squamous cell carcinoma line with IC50 of 15.1 nM.
Dacomitinib (PF-00299804, PF-299804) causes significant antitumor activity, including marked tumor regressions in a variety of human tumor xenograft models that express and/or overexpress erbB family members or contain the double mutation (L858R/T790M) in EGFR associated with resistance to gefitinib and erlotinib.

物理化学性质&存储条件

分子量 469.94
分子式 C24H25ClFN5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 50 mg/mL (Need ultrasonic)
Chemical Name/SMILES

2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-, (2E)-

参考文献

1. Engelman JA, et al. Cancer Res. 2007 Dec 15;67(24):11924-32.

2. Gonzales AJ, et al. Mol Cancer Ther. 2008 Jul;7(7):1880-9.

3. Nguyen KS, et al. Clin Lung Cancer. 2009 Jul;10(4):281-9.

4. Kalous O, et al. Mol Cancer Ther. 2012 Sep;11(9):1978-87.

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