Description
| Description | AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader specifically targeting SWI/SNF ATPase subunits, namely SMARCA2 and SMARCA4. It successfully inhibits tumor growth in xenograft models of prostate cancer with remarkable potency. Furthermore, AU-15330 exhibits synergistic effects when combined with the AR antagonist enzalutamide. Notably, AU-15330 demonstrates disease remission in models of castration-resistant prostate cancer (CRPC) without inducing any toxicities. |
| In vivo |
AU-15330 (10 and 30 mg/kg; i.v.; 5 days per week for 3 weeks) shows no evident toxicity in immuno-competent mice.[1] AU-15330 (60 mg/kg with or without 10 mg/kg enzalutamide; i.v.; 3 days per week; p.o.; 5 days per week for 5 weeks) leads to potent inhibition of tumor growth, triggering disease regression in more than 20% of animals. The combinatorial regimen induced the most potent anti-tumor effect, with regression in all animals.[1] AU-15330 (60 mg/kg with or without 10 mg/kg enzalutamide; i.v.; 3 days per week; p.o.; 5 days per week for 5 weeks) strongly inhibits the growth of C4-2B cell line-derived CRPC xenografts in intact mice as a single agent and synergized with enzalutamide.[1] AU-15330 (60 mg/kg with or without 10 mg/kg enzalutamide; i.v.; 3 days per week; p.o.; 5 days per week for 5 weeks) combines with enzalutamide induces significant tumor growth inhibition, causing regression in more than 30% of animals in the middle of CRPC variant of the MDA-PCa-146-12 PDX by tumor implantation into castrated mice.[1] |
| Molecular Weight |
755.93 |
| Formula | C39H49N9O5S |
| CAS No. | 2380274-50-8 |
Storage
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Solubility Information
DMSO: 126.0 mg/mL (166.7 mM),
Need ultrasonic
( < 1 mg/ml refers to the product slightly soluble or insoluble )
