NCIt synonyms : BiDAC Degrader CFT8634; Bifunctional Degradation Activating Compound CFT8634; BRD9-targeting Protein Degrader CFT8634; BRD9 Protein Degrader CFT8634;
NCIt definition : An orally bioavailable heterobifunctional protein degrader of bromodomain-containing
protein 9 (BRD9; sarcoma antigen NY-SAR-29; rhabdomyosarcoma antigen MU-RMS-40.8),
with potential antineoplastic activity. CFT8634 is comprised of an E3 ligase-binding
moiety and a BRD9-binding moiety. Upon oral administration, BRD9 degrader CFT8634
targets and binds to BRD9 with its BRD9-binding moiety. Upon BRD9 binding, the E3
ligase-binding moiety binds to cereblon (CRBN), a component of the CRL4-CRBN E3 ubiquitin
ligase complex, which directs proteins for destruction, resulting in the proteasome-mediated
degradation of BRD9. This leads to an inhibition of the growth of tumor cells that
rely on BRD9 for survival. BRD9, a component of one form of the Brg/Brahma-Associated
Factor (BAF) complex, is needed for the survival of certain cancer cells due to mutations.;