化合物CDKI-73 T14919

Product Introduction
Bioactivity


英文名: CDKI-73

描述: CDKI-73 是一种具有口服活性的 CDK9抑制剂，其对 CDK9、CDK1 和 CDK2 的Ki 值分别为 4 nM、4 nM 和 3 nM。CDKI-73 可下调 RNA 聚合酶 II 的磷酸化。CDKI-73 也是一种 Rab11 的抑制剂。

体外活性: CDKI-73, one of the most potent CDK9 inhibitors, against a panel of AML cell lines and samples derived from 97 patients.?CDKI-73 induced cancer cells undergoing apoptosis through transcriptional downregulation of anti-apoptotic proteins Bcl-2, Mcl-1 and XIAP by majorly targeting CDK9[3].

体内活性: CDKI-73 exhibited a favorable pharmacokinetic profile with oral bioavailability of F = 56% following a single intravenous bolus dose at 2 mg/kg and an oral dose at 10 mg/kg in mice [1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 52 mg/mL (131.83 mM)


关键字: toxicity | Inhibitor | low | AML | Acute | CDKI-73 | LS 007 | myeloid | LS007 | leukemia | CLL | Apoptosis | LS-007 | endosome | Cyclin dependent kinase | CDKI 73 | CDKI73 | inhibit | CDK

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相关库: Anti-Aging Compound Library | Anti-Breast Cancer Compound Library | Cell Cycle Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Anti-Pancreatic Cancer Compound Library | Orally Active Compound Library | Bioactive Compound Library

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