Abemaciclib-d8 (Synonyms: LY2835219-d8) |
| カタログ番号GC64280 |
Abemaciclib-d8 (LY2835219-d8) は、Abemaciclib とラベル付けされた重水素です。 Abemaciclib (LY2835219) は、CDK4 と CDK6 の IC50 値がそれぞれ 2 nM と 10 nM の選択的 CDK4/6 阻害剤です。
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Cas No.: 2088650-53-5
Sample solution is provided at 25 µL, 10mM.
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Abemaciclib-d8 (LY2835219-d8) is the deuterium labeled Abemaciclib. Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
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].
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Ku BM, et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget.•2016 Mar 22;7(12):14803-13.
[3]. Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes PLX4032 resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct;13(10):2253-63.
[4]. Gelbert LM, et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with NSC 613327. Invest New Drugs. 2014 Oct;32(5):825-37.
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