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TCS-PIM-1-4a  ≥98%

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包装规格：10mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(≥100mg/ml）
产品描述：基本信息 产品编号： T11032 产品名称： TCS-PIM-1-4a CAS: 327033-36-3   储存条件 粉末 -20℃ 四年     分子式： C11H6F3NO2S 溶于液体 -80℃ 6个月 分子量： 273.23 -20℃ 1个月 化学名：  (5E)-5-[[3-(trifluoromethyl)phenyl]methylidene]-1,3-thiazolidine-2,4-dione Solubility (25°C)：   体外:   DMSO   Ethanol   Water   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 3.6599mL 18.2996mL 36.5992mL 5mM 0.7320mL 3.6599mL 7.3198mL 10mM 0.3660mL 1.8300mL 3.6599mL   生物活性 产品描述 一种泛-Pim激酶抑制剂，可通过激活AMPK来阻断mTORC1的活性。TCS-PIM-1-4a可杀死多种髓样和淋巴样细胞系(IC50值为0.8μM至40μM)。 靶点 Pim   体外研究 TCS-PIM-1-4a (10μM;24-48 hours;6812/2 cells and Jurkat cells) treatment increases the population of cells in the G1 phase from 44.3% to 68.4% and from 56.2% to 67.1% in 6812/2 and Jurkat,respectively. S-phase cells are decreased in 6812/2,whereas only small changes are seen in Jurkat cells consistent with the lesser G1 block.TCS-PIM-1-4a (5μM;6 hours;6812/2 cells and Jurkat cells) induces cell death by the induction of apoptosis.TCS-PIM-1-4a (5μM;4-8 hours;6812/2 cells and Jurkat cells) prevents the increase in 4E-BP1 protein levels and inhibits mTOR-directed phosphorylation on Thr37/46. Cell Cycle Analysis Cell Line: 6812/2 cells and Jurkat cells Concentration: 10μM Incubation Time: 24 hours,48 hours Result: Induced cell-cycle arrest. Apoptosis Analysis Cell Line: 6812/2 cells and Jurkat cells Concentration: 5μM Incubation Time: 6 hours Result: Led to an increase in the number of the cells positive for annexin V and negative for PI from 8.25% in the control to 21.85%. Western Blot Analysis Cell Line: 6812/2 cells and Jurkat cells Concentration: 10μM Incubation Time: 4 hours,8 hours Result: Prevented the increase in 4E-BP1 protein levels and inhibited mTOR-directed phosphorylation on Thr37/46. 体内研究 TCS-PIM-1-4a (SMI-4a;60mg/kg;oral gavage;twice daily;for 21 days;nu/nu nude mice) treatment causes a significant delay in the tumor growth without any change in the weight, blood counts,or chemistries. Animal Model: 18 Nu/nu nude mice with 6812/2 murine pre–T-LBL cells Dosage: 60 mg/kg Administration: Oral gavage;twice daily;for 21 days Result: Caused a significant delay in the tumor growth.
保存条件：-20℃

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