AU-15330,2380274-50-8

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AU-15330

CAS No. : 2380274-50-8

MCE 国际站：AU-15330

产品活性：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。

研究领域：PROTAC  |  Epigenetics

作用靶点：PROTACs  |  Epigenetic Reader Domain

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.
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, causing regression in more than 30% of animals in the modle of CRPC variant of the MDA-PCa-146-12 PDX by tumour implantation into castrated mice.

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