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About This Item
Empirical Formula (Hill Notation):
C37H40N6O4 · xHCl
CAS Number:
Molecular Weight:
632.75 (free base basis)
UNSPSC Code:
41116107
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
desiccated
Quality Segment
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
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
Storage Class
11 - Combustible Solids
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
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