CDK2 degrader Cpd 1

Chemical Structure : CDK2 degrader Cpd 1

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货号: PC-24380Not For Human Use, Lab Use Only.

CDK2 degrader Cpd 1 is a potent, selective heterobifunctional CDK2 degrader with DC50 of <10 nM and Dmax>90% in TOV21G cells, 1,000-fold selectivity versus CDK1.

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生物&药学活性

CDK2 degrader Cpd 1 is a potent, selective heterobifunctional CDK2 degrader with DC50 of <10 nM and Dmax>90% in TOV21G cells, 1,000-fold selectivity versus CDK1.
Cpd 1 shows >150-fold selectivity for CDK2-cyclin E1 (IC50=1.7 nM) compared to CDK1-cyclin B1 by biochemical kinase assays
Cpd 1 significantly reduced CDK2 as well as one additional off-target protein, PIP4K2C, in approximately 8,000 proteins in PBMCs.
Cpd 1 derives enhanced CDK2 v CDK1 degradation selectivity through preferential TCF with CDK2-cyclin E1.
Cpd 1 co-degrades cyclin E1 in multiple cell types.
Cpd 1-mediated CDK2 degradation inhibitsRB-E2F pathway in CCNE1-amplified cells
Cpd 1 selectively targets CCNE1amp cancer cells and re-sensitizes palbociclib-adapted breast cells overexpressing cyclin E1.
Cpd 1 decreases cyclin E1 protein levels, in contrast to PF-07104091 which upregulates cyclin E1 protein levels, demonstrates >300-fold shift in proliferative relative IC50 from RBwt to RBKO cells.

物理化学性质&存储条件

分子量	885.48
分子式	C44H53ClN10O6S
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, 4-[(6-chloro-8-cyclopentyl-7,8-dihydro-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-methyl-N-[2-[[trans-4-[[4-[3-(tetrahydro-2,4-dioxo-1(2H)-pyrimidinyl)imidazo[1,2-a]pyridin-7-yl]-1-piperidinyl]methyl]cyclohexyl]oxy]ethyl]-

参考文献

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