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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

Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
15883
Advantage
64
ChemShuttle, Inc.
Tel
0510-83588313-811 18800520310
Email
sales@chemshuttle.com
Country
China
ProdList
2999
Advantage
62
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3506
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
Advantage
55
Jilin Province Woda Biotechnology Co., Ltd.
Tel
13504435624
Email
1927928688@qq.com
Country
China
ProdList
1615
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32435
Advantage
58
Suzhou Chenrui Biotechnology Co. LTD
Tel
17625585511
Fax
qq:1580084073
Email
1580084073@qq.com
Country
China
ProdList
959
Advantage
58
ShangHai ChuanQian Chemcial Technique Centre
Tel
15869524721
Email
3525679403@qq.com
Country
China
ProdList
4989
Advantage
58
Zhengzhou convergence chemical co., LTD
Tel
0371-0371-55153829 18003835034
Email
2853979819@qq.com
Country
China
ProdList
9998
Advantage
58
Nantong Hi-Future Biotechnology Co., Ltd
Tel
18051384581
Email
sales@chemhifuture.com
Country
China
ProdList
2995
Advantage
58

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