PROTAC CDK9 degrader-11
Product Specifications
CAS Number
3039540-19-4
Target
CDK, PROTACs
Related Pathways
Cell Cycle/Checkpoint, PROTAC
Bioactivity
PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC CDK9 degrader with a DC50 of 1.09 nM. This compound exhibits cytotoxicity in small cell lung cancer (SCLC) cells, with IC50 values in the nanomolar range. It induces cell cycle arrest at the G0/G1 phase and inhibits cell invasion in DMS114 and DMS53 cells. In addition, PROTAC CDK9 degrader-11 shows antitumor activity in an NCI-H446 xenograft mouse model. (Pink: ligand for target protein CDK9 ligand 3; Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56)
Smiles
O=C(NC1=CNN=C1C(=O)NC2CCN(C(=O)CN3CCC(CN4CCN(C=5C=CC=C(C5)NC6C(=O)NC(=O)CC6)CC4)CC3)CC2)C=7C(Cl)=CC=CC7Cl
Molecular Formula
C39H48Cl2N10O5
Molecular Weight
807.768
Shipping Conditions
Ice Packs
Storage Temperature
-20°C
Available Sizes
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