AUR1545
Based on 1 Customer Validation
AUR1545 is a selective KAT2A/KAT2B ((GCN5/PCAF)) PROTAC degrader that induces monocyte differentiation and inhibits the growth of acute myeloid leukemia cells. AUR1545 inhibits cell growth, induces epithelial differentiation and suppresses tumor growth in small cell lung cancer models. AUR1545 inhibits cell growth and induces differentiation in neuroendocrine prostate cancer cells and primary patient-derived organoids. AUR1545 is applicable to research related to acute myeloid leukemia, small cell lung cancer and neuroendocrine prostate cancer.
(Pink: GCN5/PCAF ligand (HY-W1122565); Blue: Cereblon ligand (HY-138793); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.58%
- No. CAS: 3031593-79-7
- Fòrmula: C41H50BrN9O5
- Peso molecular:828.80
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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GCN5/PCAF |
Cereblon |
AUR1545 potently degrades KAT2A/KAT2B and inhibits the growth of NCI-H1048, LASCPC-01 and MOLM-13 cells (1.5 nM, 5 nM, and 1.2 nM, respectively); its DC50 values against KAT2A in the three cell lines are 0.01 nM, 0.67 nM, and 0.11 nM respectively, while its DC50 values against KAT2B are 1.5 nM, 0.16 nM, and 0.075 nM respectively[1].
AUR1545 (0.001-100 nM; 48 h-8 d) induces differentiation in MOLM-13 cells, with an EC50 of 0.3 nM for CD86[1].
AUR1545 (0.01-100 nM; 24 h-7 d) induces epithelial differentiation in LASCPC-01 cells[1].
AUR1545 (0.01-1000 nM; 72 h-21 d) induces microglial differentiation in primary organoids derived from NEPC patients[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ASCPC-01 cells line
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Concentration:0.01 nM, 0.1 nM, 1 nM, 10 nM, 100 nM
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Incubation Time:72 h
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Result:Potently degrades KAT2A/KAT2B.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Small cell lung cancer-brearing nude balb/c mouse model[1]
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Dosage:30 mg/kg
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Administration:i.p.; once per week
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Result:Achieved 70% tumor growth inhibition (TGI); upregulated epithelial gene set enrichment analysis (GSEA) signatures in treated tumors compared to vehicle controls; reduced KAT2A and KAT2B levels significantly in tumors 168 hours post last dose.
Chemical Information
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No. CAS 3031593-79-7
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Appearance Solid
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Peso molecular 828.80
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Fòrmula C41H50BrN9O5
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Color Off-white to light yellow
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SMILES
O=C1NC(C(N2C(C3=C(C=C(C=C3)N4CCN(CC4)CC5CCN(CC5)C(C6=CC=C([C@@H]7CN(C)C[C@H](NC(C=NN8C)=C(Br)C8=O)C7)C=C6)=O)C2)=O)CC1)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (120.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (6.03 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (6.03 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.2066 mL | 6.0328 mL | 12.0656 mL | 30.1641 mL |
| 5 mM | 0.2413 mL | 1.2066 mL | 2.4131 mL | 6.0328 mL | |
| 10 mM | 0.1207 mL | 0.6033 mL | 1.2066 mL | 3.0164 mL | |
| 15 mM | 0.0804 mL | 0.4022 mL | 0.8044 mL | 2.0109 mL | |
| 20 mM | 0.0603 mL | 0.3016 mL | 0.6033 mL | 1.5082 mL | |
| 25 mM | 0.0483 mL | 0.2413 mL | 0.4826 mL | 1.2066 mL | |
| 30 mM | 0.0402 mL | 0.2011 mL | 0.4022 mL | 1.0055 mL | |
| 40 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7541 mL | |
| 50 mM | 0.0241 mL | 0.1207 mL | 0.2413 mL | 0.6033 mL | |
| 60 mM | 0.0201 mL | 0.1005 mL | 0.2011 mL | 0.5027 mL | |
| 80 mM | 0.0151 mL | 0.0754 mL | 0.1508 mL | 0.3771 mL | |
| 100 mM | 0.0121 mL | 0.0603 mL | 0.1207 mL | 0.3016 mL |
AUR1545 Related Classifications
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