NVP-2  ≥98%

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包装规格:5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性:溶于DMSO(≥ 100 mg/mL)
产品描述:基本信息 产品编号:N10621 产品名称:NVP-2 CAS: 1263373-43-8   储存条件 粉末 -20℃ 四年     分子式: C27H37ClN6O2 溶于液体 -80℃ 两年 分子量 513.07 -20℃ 一个月 化学名:  4-((5'-chloro-2'-((1R,4r)-4-((R)-1-methoxypropan-2-ylamino)cyclohexylamino)-2,4'-bipyridin-6-ylamino)methyl)tetrahydro-2H-pyran-4-carbonitrile   Solubility (25°C)   体外 DMSO 100mg/mL (194.9mM) Ethanol 100mg/mL (194.9mM) 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 1.9491mL 9.7453mL 19.4905mL 5mM 0.3898mL 1.9491mL 3.8981mL 10mM 0.1949mL 0.9745mL 1.9491mL 50mM 0.0390mL 0.1949mL 0.3898mL   生物活性 产品描述 一种有效且具有选择性的 ATP 竞争性细胞周期蛋白依赖性激酶 9 (CDK9) 探针,可抑制 CDK9/CycT 活性,IC50 值为 0.514nM。 靶点/IC50 CDK9/CycT (Cell-free assay) 0.514nM   体外研究 NVP-2 has an anti-proliferation of leukemia cells, inhibits KOPT-K1, Jurkat, P12-ICHIKAWA, DU.528, MOLT 16, HSB-2, PF-382,SKW-3, SUP-T11, DND-41 and HPB-ALL cells with IC50 values of 0.1688 µM, 0.1233 µM,0.5736 µM,0.1575 µM, 0.1620 µM,0.1585µM, 0.1808 µM, 0.2589 µM, 0.0918 µM and 0.3023 µM, respectively. NVP-2 (250 nM-1μM; 6 hours) engages CDK9 in wildtype and CRBN−/− MOLT4 cells at all concentrations, while CDK2 and CDK7 are unaffected. NVP-2 (0-10nM; 72 hours) exhibits CRBN-dependent anti-proliferative and pro-apoptotic effects in MOLT4 cells, displays an IC50 value of 9nM. NVP-2 (250nM; 24 hours) induces cell apoptosis in MOLT4 cells, upregulates caspase-3 and γH2A.X expression. However, while the compound washout significantly reduces the degree of apoptosis induced by NVP-2. Cell Viability Assay Cell Line: Leukemia cell lines Concentration: 0.1233 µM-0.5736 µM Incubation Time: 72 hours Result: Inhibited Leukemia cell lines viabity. Western Blot Analysis Cell Line: Wildtype and CRBN−/− MOLT4 cells Concentration: 1μM; 500nM; 250nM Incubation Time: 6 hours Result: Degrade CDK9  sub-stoichiometrically at all concentrations. Apoptosis Analysis Cell Line: Wildtype and CRBN−/− MOLT4 cells Concentration: 250nM Incubation Time: 24 hours Result: Induced cell apoptosis in cells and wash outed the compound relieved NVP-2-induced cell apoptosis. Cell Proliferation Assay Cell Line: MOLT4 cells Concentration: 0-10nM Incubation Time: 72 hours Result: Exhibited anti-proliferative effects in MOLT4 cells.
保存条件:-20℃