SML4290

AU-24118 hydrochloride

≥98% (HPLC)

• Synonym(e): 3-(4-(1′-(4-(3-Amino-6-(2-hydroxyphenyl)pyridazin-4-yl)phenyl)-[1,4′-bipiperidin]-4-yl)phenoxy)piperidine-2,6-dione hydrochloride, AU 24118 hydrochloride, AU24118 hydrochloride
• Empirische Formel (Hill-System): C₃₇H₄₀N₆O₄ · xHCl
• CAS-Nummer: 3084244-26-5
• Molekulargewicht: 632.75 (free base basis)
• UNSPSC Code: 41116107
• eCl@ss: 32120505
• Assay: ≥98% (HPLC)
• Form: powder
• Storage condition: desiccated

Eigenschaften

• 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

Beschreibung

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

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable