3030276-48-0
Chemical Structure
PROTAC CDK2-pRb degrader-1
- CAS No.: 3030276-48-0
- Formula:C40H50F4N8O5S
- Molecular Weight:830.93
InChIKey: LRFIOVWDBXCZHK-QDTVRVCYSA-N
SMILES: FC(F)(C1=CN=C(NC2=C(C=C(C=C2)S(N[C@H]3CC[C@@H](CC3)CN4CCN(C5=C(C=C(C6C(NC(CC6)=O)=O)C=C5)F)CC4)(=O)=O)C)N=C1N7C[C@@](O)(CCC7)C)F
Biological Activity: PROTAC CDK2-pRb degrader-1 is an orally active PROTAC-class degrader of CDK2. PROTAC CDK2-pRb degrader-1 effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811 by inducing ubiquitination and proteasomal degradation of CDK2. PROTAC CDK2-pRb degrader-1 exhibits significant activity against human cells (with EC50 values of 12 nM and 125 nM, respectively). In xenograft models, PROTAC CDK2-pRb degrader-1 effectively inhibits tumor growth and induces tumor stasis, making it suitable for research related to CCNE1-amplified cancers (such as ovarian cancer, gastric cancer, and breast cancer)[1].
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PROTAC CDK2-pRb degrader-1 | PROTAC CDK2-pRb degrader-1 is an orally active PROTAC-class degrader of CDK2. PROTAC CDK2-pRb degrader-1 effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811 by inducing ubiquitination and proteasomal degradation of CDK2. PROTAC CDK2-pRb degrader-1 exhibits significant activity against human cells (with EC50 values of 12 nM and 125 nM, respectively). In xenograft models, PROTAC CDK2-pRb degrader-1 effectively inhibits tumor growth and induces tumor stasis, making it suitable for research related to CCNE1-amplified cancers (such as ovarian cancer, gastric cancer, and breast cancer). | |||||||||||||||||||||
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