| Identification | Back Directory | [Name]
INDEX NAME NOT YET ASSIGNED | [CAS]
2380274-50-8 | [Synonyms]
AU-15330
(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 | [Molecular Formula]
C39H49N9O5S | [MOL File]
2380274-50-8.mol | [Molecular Weight]
755.94 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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.
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| 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.
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| 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.
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| [storage]
4°C, stored under nitrogen, away from moisture | [References]
[1]. Xiao L, et al. Targeting SWI/SNF ATPases in enhancer-addicted prostate cancer. Nature. 2022;601(7893):434-439. |
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| Company Name: |
ChemShuttle, Inc.
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| Tel: |
0150-83588313-811 18800520310 |
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www.jiehuapharma.com/ |
| Company Name: |
InvivoChem
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| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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