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首页-抗体药物偶连体和PROTACs-PROTAC-CDK2 degrader Cpd 5
CDK2 degrader Cpd 5

Chemical Structure : CDK2 degrader Cpd 5

CAS No.: 3030276-48-0

CDK2 degrader Cpd 5

货号: PC-24381Not For Human Use, Lab Use Only.

CDK2 degrader Cpd 5 is a potent, selective, in vivo active heterobifunctional CDK2 degrader.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CDK2 degrader Cpd 5 is a potent, selective, in vivo active heterobifunctional CDK2 degrader.
Cpd 5 drives tumor stasis in xenograft models of CCNE1amp cancer.
Cpd 5 achieves sustained 90% CDK2 degradation and 90% pRB inhibition at 30 and 50 mpk BID in HCC1569 xenograft model.
Cpd 5 induces tumor stasis in HCC1569 xenograft model at doses that give 90% RB pathway inhibition (95% TGI (p = 0.025) at 30 mg/kg and 5% regression (p < 0.001) at 50 mg/kg (Kruskal-Wallis, post-hoc Tukey). 
Cpd 5 induces 90% CDK2 degradation and 90% pRB inhibition at 50 mpk BID in MKN1 xenograft model.

物理化学性质&存储条件

分子量 830.94
分子式 C40H50F4N8O5S
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

Benzenesulfonamide, N-[trans-4-[[4-[4-(2,6-dioxo-3-piperidinyl)-2-fluorophenyl]-1-piperazinyl]methyl]cyclohexyl]-4-[[4-[(3S)-3-hydroxy-3-methyl-1-piperidinyl]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-3-methyl-

参考文献

1. Kwiatkowski N, et al. Cell Chem Biol. 2025 Apr 17;32(4):556-569.e24.

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