AU-15330

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 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Six-week-old male CB17 severe combined immunodeficiency (SCID) mice Dosage: 10 and 30 mg/kg Administration: i.v. (5 days per week for 3 weeks) Result: Showed no evident toxicity in immuno-competent mice. Animal Model: VCaP castration-resistant tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice) Dosage: 60 mg/kg with or without 10 mg/kg enzalutamide Administration: i.v. (3 days per week); p.o. (5 days per week for 5 weeks) Result: Resulted inhibition of tumor growth and triggered disease regression in more than 20% of animals. Combinatorial regimen induced the most potent anti-tumour effect, with regression in all animals. Animal Model: C4-2B non-castrated tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice) Dosage: 60 mg/kg with or without 30 mg/kg enzalutamide Administration: i.v. (3 days per week); p.o. (5 days per week for 4 weeks) Result: Strongly inhibited the growth of C4-2B cell line-derived CRPC xenografts in intact mice as a single agent and synergized with enzalutamide. Form:Solid IC50& Target:SMARCA2 and SMARCA4

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