AU-15330

Product Name: AU-15330
CAS No.: 2380274-50-8
Chemical Name: AU-15330
Synonyms: AU-15330;AU-15330 ，E1103;(2S,4R)-1-((S)-2-(2-(4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide;(2S,4R)-1-[(2S)-2-(2-{4-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]piperazin-1-yl}acetamido)-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide - [AC80811]
CBNumber: CB110386041
Molecular Formula: C39H49N9O5S
Formula Weight: 755.93
MOL File: 2380274-50-8.mol

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AU-15330 Property

Boiling point:: 1046.2±65.0 °C(Predicted)
Density: 1.310±0.06 g/cm3(Predicted)
storage temp.: 4°C, stored under nitrogen, away from moisture
solubility: DMSO : 140 mg/mL (185.20 mM; Need ultrasonic)
form: Solid
pka: 6.27±0.30(Predicted)
color: Off-white to yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML4159
Product name: AU-15330
Purity: ≥98% (HPLC)
Packaging: 1 unit
Price: $189.05
Updated: 2025/07/31

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AU-15330 Chemical Properties,Usage,Production

Uses

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[1].

Biological Activity

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[1]. 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 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[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 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[1].

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 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^[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 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^[1].

Animal Model:	Six-week-old male CB17 severe combined immunodeficiency (SCID) mice^[1]
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)^[1]
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)^[1]
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.

References

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

AU-15330 Preparation Products And Raw materials

Raw materials

Preparation Products

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AU-15330 Suppliers

China 28 United States 2 Global 30

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2380274-50-8, AU-15330Related Search:

(2S,4R)-1-((S)-2-(2-(4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

AU-15330

AU-15330 ，E1103

(2S,4R)-1-[(2S)-2-(2-{4-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]piperazin-1-yl}acetamido)-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide - [AC80811]

2380274-50-8

C39H49N9O5S