PROTAC CDK2-pRb degrader-1

SKU: orb3211143

Description

PROTAC CDK2-pRb degrader-1 is an orally bioavailable degrader belonging to the PROTAC class, specifically targeting CDK2/cyclin E complexes. It functions by promoting the ubiquitination and proteasomal degradation of CDK2, thereby effectively inhibiting the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811. PROTAC CDK2-pRb degrader-1 demonstrates significant activity in human cells with EC50 values of 12 nM and 125 nM. In xenograft models, it inhibits tumor growth and induces tumor stasis, making it suitable for research on CCNE1-amplified cancers, including ovarian, gastric, and breast cancers.

Key Properties

• CAS Number: 3030276-48-0
• MW: 830.93
• Formula: C₄₀H₅₀F₄N₈O₅S
• SMILES: C(F)(F)(F)C=1C(=NC(NC2=C(C)C=C(S(N[C@H]3CC[C@H](CN4CCN(CC4)C5=C(F)C=C(C=C5)C6C(=O)NC(=O)CC6)CC3)(=O)=O)C=C2)=NC1)N7C[C@@](C)(O)CCC7
• Target: CDK,PROTACs

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

CDK,PROTACs