BSJ-03-204 是由Cereblon配体和CDK配体相连的PROTAC，是一种有效的，选择性的基于 Palbociclib (HY-50767) 的CDK4/6双重降解剂，对 CDK4/D1 和 CDK6/D1 的IC50分别为 26.9 nM 和 10.4 nM。BSJ-03-204 不诱导 IKZF1/3 降解，具有抗癌活性。
| 生物活性 | BSJ-03-204 is aPROTACconnected by ligands forCereblonandCDK. BSJ-03-204 is a potent and selective Palbociclib-basedCDK4/6dual degrader (PROTAC), withIC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity[1]. |
| IC50& Target[1] | CDK4/D1 26.9 nM (IC50) | CDK6/D1 10.4 nM (IC50) |
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体外研究
(In Vitro) | BSJ-03-204 (0.0001-100 μM; for 3 or 4 days) has potent anti-proliferative effects on MCL cell lines[1].
BSJ-03-204 (1 μM; for 1 day) potently induces a G1 arrest[1].
BSJ-03-204 (0.1-5 μM; for 4 hours) only resultes in degradation of CDK4/6 in WT cells, not IKZF1/3[1].
Cell Proliferation Assay[1] | Cell Line: | MCL cell lines (Jeko-1, Mino, Granta-519, Rec-1, and Maver-1 cells) | | Concentration: | 0.0001-100 μM | | Incubation Time: | For 3 or 4 days | | Result: | Had potent anti-proliferative effects on mantle cell lymphoma (MCL) cell lines. |
Cell Cycle Analysis[1] | Cell Line: | Granta-519 cells | | Concentration: | 1 μM | | Incubation Time: | For 1 day | | Result: | Potently induced a G1 arrest. |
Western Blot Analysis[1] | Cell Line: | Wildtype (WT) or Crbn-/-Jurkat cells | | Concentration: | 0.1, 0.5, 1, 5 μM | | Incubation Time: | For 4 hours | | Result: | Only resulted in degradation of CDK4/6 in WT cells, not IKZF1/3. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(120.06 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.2006 mL | 6.0031 mL | 12.0062 mL | | 5 mM | 0.2401 mL | 1.2006 mL | 2.4012 mL | | 10 mM | 0.1201 mL | 0.6003 mL | 1.2006 mL |
*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。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
