产品说明书
BSJ-03-123
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同义名 : | BSJ |
| CAS号 : | 2361493-16-3 | |
| 货号 : | A1148285 | |
| 分子式 : | C47H56N10O11 | |
| 纯度 : | 98+% | |
| 分子量 : | 937.01 | |
| MDL号 : | MFCD31813815 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(112.06 mM)，配合低频超声，并调节pH至3，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | BSJ-03-123 is a PROTAC selectively targeting on CDK6, consist of a warhead palbociclib (a CDK inhibitor) linked to a CRBN ligand pomalidomide. BSJ-03-123 led a cellular degradation of CDK6, but not CDK4, at concentration ranging in 50-1000nM post 3h and resulted a time-dependent depletion of CDK6 at concentration of 200nM within 3h. BSJ-03-123 exploited homolog-selective dependency on CDK6 as it caused a potent anti-proliferative effect on CDK6-dependent AML cell lines, such as H358, by inducing a G1 cell-cycle arrest without a measurable increase in apoptosis. Selective depletion of CDK6 by 200nM BSJ-03-123 decreased phosphorylation level of Rb on site S780 which is catalyzed by CDK4/6[1]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.07mL 0.21mL 0.11mL |
5.34mL 1.07mL 0.53mL |
10.67mL 2.13mL 1.07mL |
| 参考文献 |
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