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首页-抗体药物偶连体和PROTACs-PROTAC-CDK2 degrader CPS2
CDK2 degrader CPS2

Chemical Structure : CDK2 degrader CPS2

CAS No.: 2756741-90-7

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CDK2 degrader CPS2 (CPS2)

货号: PC-49057Not For Human Use, Lab Use Only.

CDK2 degrader CPS2 is a potent, selective CDK2 degarder (PROTAC) with IC50 of 24 nM, potently and specifically induces CDK2 degradation in various cancer cell lines (MDA-MB-231, DC50=8 nM; MV-4-11, DC50=1 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CDK2 degrader CPS2 is a potent, selective CDK2 degarder (PROTAC) with IC50 of 24 nM, potently and specifically induces CDK2 degradation in various cancer cell lines (MDA-MB-231, DC50=8 nM; MV-4-11, DC50=1 nM).
CPS2 induced ubiquitination led to CDK2 degradation via the ubiquitin/proteasome system, this degradation required the binding of CPS2 to CDK2 and CRBN.
CPS2 did not directly perturb the other CDK proteins (such as CDK1, 4, 5, 6, 7, 8 and 9) under subnanomolar concentration conditions.
CPS2 induced AML cell differentiation, increased CD11b expression in a concentration-dependent manner in the NB4 cells, also promoted ATRA-induced CD11b upregulation in the HL60 cells.
CPS2 inhibited the proliferation of hematopoietic stem cells (HSCs) without inducing cytotoxicity, CPS2 also induced granulocytic differentiation of HSCs.

物理化学性质&存储条件

分子量 890.948
分子式 C38H42N12O10S2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4-((5-amino-1-(3-methylthiophene-2-carbonyl)-1H-1,2,4-triazol-3-yl)amino)-N-(2-((1-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)methoxy)ethyl)benzenesulfonamide

参考文献

1. Wang L, et al. Nat Chem Biol. 2021 May;17(5):567-575.

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