Amredobresib
Based on 1 Customer Validation
Amredobresib (BI894999) is an orally active BET inhibitor. Amredobresib inhibits the binding of BRD4-BD1 and BRD4-BD2 bromodomains to acetylated histones with IC50 values of 5 nM and 41 nM, respectively. Amredobresib exhibits anticancer activity against acute myeloid leukemia (AML) and NUT cancer.
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。
The Amredobresib was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- 純度: 98.97%
- CAS 番号: 1610044-98-8
- 分子式: C26H29N9
- 分子量:467.57
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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
生物活性
BET[1]
Amredobresib inhibits the proliferation of NUT carcinoma (NC) cell lines[3].
Amredobresib (10-30 nM; 30 min) causes the rapid detachment of BRD4-NUT from chromatin in NC cell line Ty-82[3].
Amredobresib (3.3-30 nM; 24-72 h) causes G1 arrest in MV-4-11B cells[4].
Amredobresib inhibits the binding of the BRD4-BD1 and BRD4-BD2 bromodomains to acetylated histones with IC50 values of 5 nM and 41 nM, respectively[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Amredobresib (2-4 mg/kg; p.o.; daily) inhibits tumor growth and prolongs survival in mouse models engrafted intravenously with human MV-4-11B AML cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-8 week old, female CIEA-NOG mice (NOD.Cg-PrkdcscidIL2rgtm1Sug/JicTac) engrafted intravenously with human luciferase labeled MV-4-11B cells[4]
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Dosage:2 mg/kg or 4 mg/kg
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Administration:Oral gavage (p.o.); daily
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Result:Resulted in tumor growth inhibition (TGI) of 96% and survival prolongation of 29.5 days at 2 mg/kg.
Resulted in a TGI of 99% and survival prolongation of 52 days at 4 mg/kg.
化学情報
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CAS 番号 1610044-98-8
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性状 Solid
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分子量 467.57
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分子式 C26H29N9
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Color Light yellow to yellow
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SMILES
CNC1=NC(C2=NC3=C(N2CC4=CC=CC=C4)C=C(N5CCN(CC5)C)C=C3)=CN6C(C)=NN=C16
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別名
BI894999
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
DMSO : 0.5 mg/mL (1.07 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)
DMSO : 0.5 mg/mL (1.07 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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)
純度とドキュメンテーション
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データシート (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Ulrike Tontsch-Grunt, et al. Combination treatment of acute myeloid leukemia. Patent WO2019145410A1.
[2]. Shaonan Wang, et al. Method for administration of an anti cancer agent. Patent WO2021175824A1.
[3]. Tontsch-Grunt U, et al. Therapeutic impact of BET inhibitor BI 894999 treatment: backtranslation from the clinic. Br J Cancer. 2022 Aug;127(3):577-586. [Content Brief]
[4]. Tontsch-Grunt U, et al. Synergistic activity of BET inhibitor BI 894999 with PLK inhibitor volasertib in AML in vitro and in vivo. Cancer Lett. 2018 May 1;421:112-120. [Content Brief]
[5]. Gerlach D, et al. The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML. Oncogene. 2018 May;37(20):2687-2701. [Content Brief]
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 (sealed storage, away from moisture and light). 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 / DMSO | 1 mM | 2.1387 mL | 10.6936 mL | 21.3872 mL | 53.4679 mL |
Amredobresib 関連分類
HY-145550 関連分類
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