AU-15330

Research use only, not for human use.

AU-15330 is a proteolytic targeting chimera (PROTAC) that simultaneously targets SMARCA4, SMARCA2, and PBRM1 for degradation and exhibits cytotoxicity in H3.3K27M cells but not in H3 wild-type cells.

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.

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Animal Model:Six-week-old male CB17 severe combined immunodeficiency (SCID) miceDosage: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 enzalutamideAdministration: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.

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Others

Other Targets

PROTACs | Epigenetic Reader Domain

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2380274-50-8

755.93

C39H49N9O5S

>98% (HPLC)

In Vitro:?DMSO : 140 mg/mL (185.20 mM; Ultrasonic )

C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](NC(=O)CN1CCN(CC1)c1cc(nnc1N)-c1ccccc1O)C(C)(C)C)c1ccc(cc1)-c1scnc1C

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(-20℃)

With Ice Pack

≥ 2 years