| 中文名称: | PIM447 | ||||
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| 英文名称: | PIM447 | ||||
| 别名: | PIM447 PIM447 | ||||
| CAS No: | 1210608-43-7 | 分子式: | C24H23F3N4O | 分子量: | 440.46 |
| CAS No: | 1210608-43-7 | ||||
| 分子式: | C24H23F3N4O | ||||
| 分子量: | 440.46 | ||||
基本信息
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产品编号： |
P11241 |
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产品名称： |
PIM447 |
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CAS: |
1210608-43-7 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
二年 |
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分子量： |
440.46 |
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化学名： |
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Solubility (25°C)： |
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体外:
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DMSO |
88mg/mL (184.51mM) |
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Ethanol |
88mg/mL (184.51mM) |
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Water |
Insoluble |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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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。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.0968mL |
10.4839mL |
20.9679mL |
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5mM |
0.4194mL |
2.0968mL |
4.1936mL |
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10mM |
0.2097mL |
1.0484mL |
2.0968mL |
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50mM |
0.0419mL |
0.2097mL |
0.4194mL |
生物活性
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产品描述 |
一种有效的、口服的、选择性的泛PIM激酶抑制剂,具有双重抗肿瘤和骨保护作用。PIM447诱导细胞凋亡。 |
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靶点 |
Pim1 |
Pim3 |
Pim2 |
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6pM(Ki) |
9pM(Ki) |
18pM(Ki) |
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体外研究 |
PIM447 (0.05-10 μM; 24-72 hours) shows antiproliferative effect on the multiple myeloma (MM) cells.PIM447 (10 μM; 6-24 hours) induces apoptosis.PIM447 (0.1-10μM; 48 hours) increases the percentage of cells in the G0-G1 phase and decreases the proliferative phases (Sand G2–M) of the cell cycle, in the two cell lines (MM1S and OPM-2 cells) at all doses. Cell Viability Assay |
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Cell Line: |
MM1S,MM1R,RPMI-8226,MM144,U266,NCI-H929,OPM-2,RPMI-LR5,U266-Dox4,and U266-LR7 cells |
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Concentration: |
0.05,0.1,0.5,1,5,10μM |
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Incubation Time: |
24,48,72 hours |
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Result: |
Sensitive cell lines with IC50 values at 48 hours 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 48 hours >7 μmol/L (OPM-2,RPMI-LR5,U266-Dox4,and U266-LR7). |
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Western Blot Analysis |
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Cell Line: |
MM1S cells |
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Concentration: |
10μM |
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Incubation Time: |
6,12,24 hours |
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Result: |
Promoted the cleavage of initiator caspases,such as caspases 8 and 9,and also the cleavage of the effector caspases 3 and 7,together with PARP cleavage. |
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体内研究 |
PIM447 (100mg/kg;p.o.;5 times for a week) reduces tumor burden. |
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Animal Model: |
6-week-old female NOD-SCID-IL-2Rγ−/−(NSG) mice (bearing RPMI-8226-luc cells). |
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Dosage: |
100mg/kg |
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Administration: |
p.o.;5 times for a week |
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Result: |
Clearly controlled tumor progression as measured by bioluminescence. |
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推荐实验方法(仅供参考)
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细胞实验: |
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细胞系 |
KG-1细胞 |
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浓度 |
0.05,0.5和5μM |
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处理时间 |
2h |
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方法 |
用一定浓度的PIM447处理KG-1细胞2小时后，将细胞置于RIPA buffer中进行裂解。用BCA法检测蛋白质浓度，将50μg溶解产物用SDS-PAGE法进行分离、电泳。然后将蛋白转移至0.2μm硝酸纤维膜（转膜），WB检测pS6RP/总S6RP的表达量。 |
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动物实验: |
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动物模型 |
KG-1 AML xenograft mouse model |
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剂量 |
30或100mg/kg |
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给药处理 |
口服 |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
