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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
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.
- Purity: 98.97%
- CAS No.: 1610044-98-8
- 화학식: C26H29N9
- 분자량:467.57
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보관:
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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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분자량 467.57
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
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)
용액&용해도
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)
순도&문서
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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 |
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