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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。
BSJ-03-204图片
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 mg5 mg10 mg
1 mM1.2006 mL6.0031 mL12.0062 mL
5 mM0.2401 mL1.2006 mL2.4012 mL
10 mM0.1201 mL0.6003 mL1.2006 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。