| Company Name: |
ChemShuttle, Inc.
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| Tel: |
0510-83588313-802 18800520310; |
| Email: |
sales@chemshuttle.com |
| Products Intro: |
Product Name:(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
CAS:2380274-50-8
Purity:95% Package:5mg;25mg;100mg;500mg;1g;5g;10g;25g;50g;100g;250g;500g;kg…
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| | INDEX NAME NOT YET ASSIGNED Basic information |
| Product Name: | INDEX NAME NOT YET ASSIGNED | | Synonyms: | (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 | | CAS: | 2380274-50-8 | | MF: | C39H49N9O5S | | MW: | 755.94 | | EINECS: | | | Product Categories: | | | Mol File: | 2380274-50-8.mol |  |
| | INDEX NAME NOT YET ASSIGNED Chemical Properties |
| 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 |
| | INDEX NAME NOT YET ASSIGNED Usage And Synthesis |
| 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]. | | References | [1]. Xiao L, et al. Targeting SWI/SNF ATPases in enhancer-addicted prostate cancer. Nature. 2022;601(7893):434-439. |
| | INDEX NAME NOT YET ASSIGNED Preparation Products And Raw materials |
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