Chemical Structure : CDK2 degrader Cpd 5
CAS No.:
3030276-48-0
CDK2 degrader Cpd 5
Catalog No.: PC-24381Not For Human Use, Lab Use Only.
CDK2 degrader Cpd 5 is a potent, selective, in vivo active heterobifunctional CDK2 degrader.
Bulk size, bulk discount!
Welcome credit card payment!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
|
M.Wt
|
830.94
|
|
Formula
|
C40H50F4N8O5S
|
|
Appearance
|
Solid
|
|
CAS No.
|
|
|
Storage
|
- Solide Powder
-
-20°C 12 Months; 4°C 6 Months
|
- In Solvent
-
-80°C 6 Months; -20°C 6 Months
|
|
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-
|
References
1. Kwiatkowski N, et al. Cell Chem Biol. 2025 Apr 17;32(4):556-569.e24.
Contact Us
sales@probechem.com
