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PIM-447 dihydrochloride  ≥98%

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包装规格：1mg 5mg 10mg 50mg in glass bottle
溶解性：溶于DMSO（≥ 46.7 mg/mL）
产品描述：基本信息 产品编号： P10799 产品名称： PIM-447 dihydrochloride CAS: 1820565-69-2   储存条件 粉末 -20℃ 四年     分子式： C24H25Cl2F3N4O 溶于液体 -80℃ 6个月 分子量： 513.38 -20℃ 1个月 化学名：  2-Pyridinecarboxamide,N-[4-[(1R,3S,5S)-3-amino-5-methylcyclohexyl]-3-pyridinyl]-6-(2,6-difluorophenyl)-5-fluoro-,hydrochloride (1:2) 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 1.9479mL 9.7394mL 19.4787mL 5mM 0.3896mL 1.9479mL 3.8957mL 10mM 0.1948mL 0.9739mL 1.9479mL   生物活性 产品描述 一种有效的、口服的、选择性的泛PIM激酶抑制剂，对PIM1、PIM2和PIM3 的Ki值分别为6、18和9pM。 靶点 Ki:6pM (PIM1);18pM (PIM1);9pM (PIM3)   体外研究 PIM-447 (0.05-10µM;24,48 and 72 hours) has inhibitory effects in MM cells,it against sensitive cell lines with IC50 values ranging from 0.2 to 3.3µM (MM1S,MM1R,RPMI-8226,MM144,U266 and NCI-H929) and less sensitive cell lines with IC50 values at 48h>7µM (OPM-2,RPMI-LR5,U266-Dox4 and U266-LR7).PIM-447 (0.1-10µM;24,48 and 72 hours) does not induce important levels of apoptosis,when PIM447 at 5µM,it substantially increases annexin-V levels (about 30%) in sensitive cell lines(MM1S,NCI-H929 and RPMI-8226).When PIM447 at 10µM,it induces apoptosis in all the cell lines but to a lesser extent in OPM-2 and RPMI-LR5.PIM447 promotes the cleavage of initiator caspases,such as caspases 8 and 9,and increases the cleavage of the effector caspases 3 and 7,together with PARP cleavage in MM1S,RPMI-8226 and NCI-H929 cells.PIM447 (0.1-1µM) increases the percentage of cells in the G0/G1 phase and decreases the proliferative phases (S and G2/M) of the cell cycle.The effects at low concentrations (0.1-1µM) were more pronounced in MM1S cells than in OPM-2. Cell Viability Assay Cell Line: Sensitive MM cell lines:MM1S,MM1R,RPMI-8226,MM144,U266 and NCI-H929 cells Less sensitive MM cell lines:OPM-2,RPMI-LR5,U266-Dox4 and U266-LR7cells Concentration: 0.05-10µM Incubation Time: 24,48 and 72 hours Result: Was cytotoxic for MM cells (PIM kinases highly expressed). Apoptosis Analysis Cell Line: Sensitive MM cell lines:MM1S,NCI-H929 and RPMI-8226 cells Less sensitive MM cell lines:OPM-2 and RPMI-LR5 cells Concentration: 0.05-10µM Incubation Time: 24,48 and 72 hours Result: Induced cell apoptosis at higer doses, had no effects at 0.1-1uM. Western Blot Analysis Cell Line: Sensitive MM cell lines:MM1S,NCI-H929 and RPMI-8226 cells Concentration: 0.05-10µM Incubation Time: 24, 48 hours Result: Increased the cleavage of the effector caspases 3 and 7,and the PARP cleavage. Cell Cycle Analysis Cell Line: MM1S,OPM-2 cells Concentration: 0.1,0.5 or 1µM Incubation Time: 48 hours Result: Increased the cleavage of the effector caspases 3 and 7,and the PARP cleavage. 体内研究 PIM447 (oral gavage;100mg/kg;5 times/week) clearly controlls tumor progression and the serum levels of hIgλ secreted by RPMI-8226-luc cells in mouse model of bone marrow-disseminated human multiple myeloma. Animal Model: RPMI-8226-luc cells are injected intravenously into 6-week-old female NODSCID-IL-2Rγ-/-(NSG) mice. Dosage: 100mg/kg Administration: oral gavage;100mg/kg;5 times/week Result: Was well tolerated,as the body weight of mice did not decrease by more than 10%.Increased bone volume density and trabecular number and reduced trabecular separation relative to vehicle group.
保存条件：-20℃

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