Lapatinib-d4-1(Synonyms: GW572016-d4-1; GW2016-d4-1)

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。
Lapatinib-d4-1 (Synonyms: GW572016-d4-1; GW2016-d4-1)

Lapatinib-d4-1 是 Lapatinib 氘代物。Lapatinib (GW572016) 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-d4-1(Synonyms: GW572016-d4-1;  GW2016-d4-1)

Lapatinib-d4-1 Chemical Structure

CAS No. : 1184264-15-0

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生物活性

Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) 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

585.08

Formula

C29H22D4ClFN4O4S

CAS 号

1184264-15-0

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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