AU-15330 是 SWI/SNF ATP 酶亚基 SMARCA2 和 SMARCA4 的蛋白水解靶向嵌合体 (PROTAC) 降解剂。AU-15330 在前列腺癌异种移植模型中诱导有效抑制肿瘤生长，并与 AR 拮抗剂 enzalutamide 协同作用。AU-15330 在去势抵抗性前列腺癌 (CRPC) 模型中诱导疾病缓解而无毒性。

AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity.

Solid

SMARCA2 and SMARCA4

AU-15330 (10 and 30 mg/kg; i.v.; 5 days per week for 3 weeks) shows no evident toxicity in immuno-competent mice.
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 tumour growth, triggering disease regression in more than 20% of animals. Combinatorial regimen induced the most potent anti-tumour effect, with regression in all animals.
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.
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 tumour growth inhibition,

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

[1]. Xiao L, et al. Targeting SWI/SNF ATPases in enhancer-addicted prostate cancer. Nature. 2022;601(7893):434-439.

In Vitro: DMSO : 140 mg/mL (185.20 mM; Need ultrasonic)配制储备液