Dacomitinib-d5(Synonyms: PF-00299804-d5; PF-299804-d5)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物，专注于信号通路和疾病研究领域。
Dacomitinib-d5 (Synonyms: PF-00299804-d5; PF-299804-d5)

Dacomitinib-d5 (PF-00299804-d5) 是 Dacomitinib 的氘代物。Dacomitinib (PF-00299804) 是一种特异，不可逆的 ERBB 家族抑制剂，作用于 EGFR，ERBB2 和 ERBB4 的 IC₅₀ 分别为 6 nM，45.7 nM 和 73.7 nM。

Dacomitinib-d5 Chemical Structure

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生物活性	Dacomitinib-d5 (PF-00299804-d5) is the deuterium labeled Dacomitinib. Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC₅₀s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively^[1].
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	474.97
Formula	C₂₄H₂₀D₅ClFN₅O₂
中文名称	达克替尼 d5
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Engelman JA, et al. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to ZD1839. Cancer Res. 2007 Dec 15;67(24):11924-32. [3]. Kalous O, et al. Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to Anti-Human HER2 and GW572016. Mol Cancer Ther. 2012 Sep;11(9):1978-87.

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