BSJ-03-204

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BSJ-03-204

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2349356-09-6

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

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)

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.

分子量

832.90

性状

Solid

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℃, 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。