AU-24118
Based on 2 publication(s) in Google Scholar
AU-24118 is a selective and orally bioavailable PROTAC degrader of mSWI-SNF ATPases (SMARCA2 and SMARCA4) and PBRM1. AU-24118 integrates a bait moiety binding to the bromodomains of SMARCA2 and SMARCA4, along with a ligand moiety for CRBN ligase. AU-24118 demonstrates tumor regression in prostate cancer model. AU-24118 can be studied to combat prostate cancer. (Pink: PBRM1/SMARCA2,4 ligand (HY-171774); Blue: CRBN ligand (HY-171775)).
(Pink: Epigenetic Reader Domain ligand (HY-171774); Blue: Ligands for E3 Ligase ligand (HY-171775); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.82%
- CAS 番号: 3084244-26-5
- 分子式: C37H40N6O4
- 分子量:632.75
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Epigenetics Compound Library
HY-L005
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Histone Modification Research Compound Library
HY-L024
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Anti-Cancer Compound Library
HY-L025
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Orally Active Compound Library
HY-L061
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Anti-Blood Cancer Compound Library
HY-L079
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Transcription Factor-Targeted Library
HY-L090
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Anti-Prostate Cancer Compound Library
HY-L124
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PROTAC Library
HY-L151
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Anti-Hematopathy Compound Library
HY-L171
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
MedChemExpress（MCE）の使用を引用している文献 AU-24118
MorePROTACs アイソフォーム固有の製品をすべて表示
MoreSWI/SNF Complex アイソフォーム固有の製品をすべて表示
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生物活性
AU-24118 (3-30 nM, 4 h) demonstrates comparable degradation efficacy of SMARCA4 and PBRM1 in VCaP prostate cancer cells[1].
AU-24118 (1 μM, 2 h) selectively degrades SMARCA2, SMARCA4, and PBRM1, resulting in their significant downregulation in VCaP cells[1].
AU-24118 (0.1 μM, 4 h) degrades SMARCA2 and PBRM1 in AUR-1 and AUR-2 cells, but is unable to degrade SMARCA4 in AUR-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:VCaP cell line-derived xenograft model
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Concentration:15 mg/kg
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Incubation Time:5 d
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Result:Downregulated SMARCA2, SMARCA4 and PBRM1 as well as specific prostate cancer lineage proteins (AR, ERG, C-Myc, and PSA) after 5 day with AU-24118 alone or with Enzalutamide (HY-70002).
| Species | Dose | Route | AUC | Tmax |
|---|---|---|---|---|
| Mice | 10 mg/kg | p.o. | 4929 ng·h/mL | 6 h |
| Mice | 100 mg/kg | p.o. | 32178 ng·h/mL | 4 h |
| Mice | 30 mg/kg | p.o. | 14716 ng·h/mL | 3 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old CB17 (male) SCID mice injected with 3 x 106 VCaP cells (s.c.) into the dorsal flank on both sides in a 1:1 mixture of serum free medium[1]
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Dosage:15 mg/kg
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Administration:Oral gavage (p.o.), 3 times per week
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Result:Downregulated SMARCA2, SMARCA4, and PBRM1 and specific prostate cancer lineage proteins including AR, ERG, C-Myc and Ki-67.
Induced apoptosis as evidenced by increased cleaved PARP levels.
Did not lead to significant body weight changes, indicating the mice tolerated AU-24118 with or without the addition of Enzalutamide.
化学情報
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CAS 番号 3084244-26-5
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性状 Solid
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分子量 632.75
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分子式 C37H40N6O4
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Color Light yellow to brown
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SMILES
NC1=C(C=C(N=N1)C2=C(C=CC=C2)O)C3=CC=C(C=C3)N4CCC(CC4)N5CCC(CC5)C6=CC=C(C=C6)OC7CCC(NC7=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell
2026 Jun 11;189(12):3541-3552.e18. PMID: 41999746 -
溶剤 & 溶解度
DMSO : 8.33 mg/mL (13.16 mM; ultrasonic and warming and heat to 60°C; 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 0.83 mg/mL (1.31 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (1.31 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 50% PEG300 50% Saline
Solubility: 12.5 mg/mL (19.76 mM); Suspended solution; Need ultrasonic
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.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
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- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5804 mL | 7.9020 mL | 15.8040 mL | 39.5101 mL |
| 5 mM | 0.3161 mL | 1.5804 mL | 3.1608 mL | 7.9020 mL | |
| 10 mM | 0.1580 mL | 0.7902 mL | 1.5804 mL | 3.9510 mL |
AU-24118 関連分類
HY-163410 関連分類
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