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CDKI-73  98.1942%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（≥ 52 mg/mL 超声）
产品描述：基本信息 产品编号：C10824 产品名称：CDKI-73 CAS: 1421693-22-2   储存条件 粉末 2-8℃ 四年 分子式： C15H15FN6O2S2 溶于液体 -80℃ 两年 分子量 394.45 -20℃ 一个月 化学名：  3-((5-fluoro-4-(4-methyl-2-(methylamino)thiazol-5-yl)pyrimidin-2-yl)amino)benzenesulfonamide   Solubility (25°C)   体外 DMSO 79mg/mL (200.27mM) Ethanol 1.5mg/mL (3.8mM) Water Insoluble 体内 现配现用   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。     制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.5352mL 12.6759mL 25.3518mL 5mM 0.5070mL 2.5352mL 5.0704mL 10mM 0.2535mL 1.2676mL 2.5352mL 50mM 0.0507mL 0.2535mL 0.5070mL     生物活性 产品描述 具有口服活性的、高效的 CDK9 抑制剂，其对CDK9、CDK1 和 CDK2 的 Ki 值分别为 4nM、4nM 和 3nM。 靶点/IC50 CDK2 (Cell-free assay) CDK9 (Cell-free assay) CDK1 (Cell-free assay) CDK4 (Cell-free assay) 3.27nM 5.78nM 8.17nM 8.18nM   体外研究 CDKI-73 is highly cytotoxic to primary leukemia cells derived from CLL patients (mean LD50 = 0.08μM) and shows>500-fold selectivity for primary leukemia cells over normal B-lymphocytes (LD50 = 40.5μM). CDKI-73 (0.1μM, 4 h) inhibits the phosphorylation of serine 2 of RNA polymerase II and MCL1 protein expression in CLL cells. CDKI-73 induced caspase-dependent apoptosis that was preceded by dephosphorylation of cdk9 and serine 2 of RNA polymerase II. CDKI-73 is highly effective against all cell lines tested with an IC50 in the range of 0.012-0.517μM; in particular three MLLAML cell lines, namely MOLM13, MV4-11 and THP-1, were highly sensitive to CDKI-73 with IC50 values <0.062μM. Cell Viability Assay. Cell Line: CLL cells. Concentration: 0-1μM. Incubation Time: 48 h. Result: Shows preferential cytotoxicity in CLL cells.   体内研究 CDKI-73 (25, 50, 100 mg/kg) markedly decreases tumor growth in a dose-dependent manner and results in a prolongation of animal life span (P < 0.001) without causing body weight loss and other overt toxicities. Animal Model: MV4-11 tumor bearing mice . Dosage: 25mg/kg. Administration: Orally once everyday for 33 days. Result: Caused a remarkable delay in tumor growth compared to vehicle-treated mice, as reflected in a percentage for the mean tumor volume in treated to control mice of 43% at day 31.   Animal Model: Balb/C mice aged 6-8 weeks. Dosage: 2mg/kg (IV), 10, 20 and 40mg/kg (PO). (Pharmacokinetic Analysis.) Administration: IV and PO, single dose. Result: The Cmax increased from 1.29 to 3.66μM at a mean time of 1 h and the area under the curve (AUC) of CDKI-73 increased from 3.51 to 12.8μM.h when the oral dose was escalated from 10 to 40mg/kg. CDKI-73 was eliminated from plasma with a mean terminal half-life (T1/2) of 2 h. Its oralbioavailability (F) ranged from 54 to 85% across the three doses.
保存条件：2-8℃ 充氮保存

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