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.
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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.
- Pureté: 98.97%
- CAS No.: 1610044-98-8
- Formule: C26H29N9
- Masse moléculaire:467.57
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Stockage:
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
Chemical Information
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CAS No. 1610044-98-8
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Appearance Solid
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Masse moléculaire 467.57
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Formule 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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Synonyms
BI894999
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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)
Solvant et solubilité
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
[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 Related Classifications
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