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Biochem/physiol Actions
AU-24118 is an orally active, potent and selective SWI/SNF ATPase degrader composed of an E3 ligase cereblon (CRBN) ligand linked to the SMARCA2/4 and PBRM1 (PB1)-selective bromodomain (BrD) inhibitor SGC-SMARCA-BRDVIII. AU-24118 induces near complete degradation of cellular SMARCA2/4 and PBRM1 (4-8h, 100 nM, 22Rv1 cells) and blocks SWI/SNF-dependent survival in cancer cultures (IC50 <100 nM post 5-day treatment; C42B, LNCaP, 22Rv1, VCaP). AU-24118 induces tumor regression in a castration-resistant prostate cancer (CRPC) VCaP xenograft model (15 mg/kg 3x/wk via p.o.) and is enhanced with concurrent AR antagonist enzalutamide treatment (10 mg/kg 5x/wk via p.o.).
Disclaimer
Hygroscopic, store with desiccant
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| storage condition | desiccated |
| color | light yellow to orange |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | -10 to -25°C |
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