Lapatinib-d7 dihydrochloride(Synonyms: GW572016-d7 dihydrochloride; GW2016-d7 dihydrochloride)

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Lapatinib-d7 dihydrochloride (Synonyms: GW572016-d7 dihydrochloride; GW2016-d7 dihydrochloride)

Lapatinib-d7 (GW572016-d7) dihydrochloride 是 Lapatinib dihydrochloride 的氘代物。Lapatinib (GW572016) dihydrochloride 是一种 ErbB-2EGFR 酪氨酸激酶结构域的有效抑制剂,对纯化的 EGFRErbB-2IC50 值分别为 10.2 和 9.8 nM。

Lapatinib-d7 dihydrochloride(Synonyms: GW572016-d7 dihydrochloride; GW2016-d7 dihydrochloride)

Lapatinib-d7 dihydrochloride Chemical Structure

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生物活性

Lapatinib-d7 (GW572016-d7) dihydrochloride is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, 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

661.02

Formula

C29H21D7Cl3FN4O4S

中文名称

拉帕替尼 d7 (双盐酸盐)

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]. Rusnak DW, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94

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