BSJ-03-204

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BSJ-03-204  纯度: 98.34%

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。

BSJ-03-204

BSJ-03-204 Chemical Structure

CAS No. : 2349356-09-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5310 In-stock
5 mg ￥3500 In-stock
10 mg ￥5800 In-stock
25 mg ￥11000 In-stock
50 mg ￥17000 In-stock
100 mg ￥25000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

BSJ-03-204 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Transcription Factor Targeted Library

生物活性

BSJ-03-204 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s 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)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

832.90

Formula

C43H48N10O8
CAS 号

2349356-09-6
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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Baishan Jiang, et al. Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6. Angew Chem Int Ed Engl. 2019 May 6;58(19):6321-6326.

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