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