AU-19820
/ Dr. Reddy’s
- LARVOL DELTA
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March 11, 2021
[VIRTUAL] Orally bioavailable SMARCA2 degraders with exceptional selectivity and potency
(AACR 2021)
- "The lead compound, AU-19820 showed > 10000-fold selectivity for SMARCA2 degradation versus other homologous proteins in tested cell lines... Potent and extremely selective SMARCA2 protein degraders were identified by conjugating SMARCA2/4 inhibitors with known VHL or CRBN ligands. SMARCA2 vs SMARCA4 selectivity handles have been very well explored with expandable SAR. Lead compound also displayed a synthetic lethality phenotype in SMARCA4 mutant cancer models while sparing SMARCA2/4 proficient ones."
Colon Cancer • Colorectal Cancer • Gastrointestinal Cancer • Glioma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Skin Cancer • Solid Tumor • CRBN • SMARCA2 • SMARCA4
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