I-BET 762
Tocris Bioscience, part of Bio-Techne | Catalog # 6521
Potent and high affinity BET bromodomain inhibitor; anti-inflammatory; orally bioavailable.
Key Product Details
Description
Potent and high affinity BET bromodomain inhibitor; anti-inflammatory; orally bioavailable.
Alternative Names
GSK525762A,Molibresib
Product Description
I-BET 762 is a potent and high affinity BET bromodomain inhibitor (IC50 = 32.5 - 42.5 nM; Kd = 50.5 - 61.3 nM). Inhibits myeloma cell proliferation. Attenuates transcription of oncogenic MYC and suppresses key inflammatory genes. Exhibits efficacy in a range of oncology and immunoinflammatory models. Displays antiproliferative effect in vitro and in vivo. Orally bioavailable.Product Specifications
Molecular Weight
423.90
Formula
C22H22ClN5O2
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
(4S)-6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide
CAS Number
1260907-17-2
PubChem ID
46943432
InChI Key
AAAQFGUYHFJNHI-SFHVURJKSA-N
SMILES
CCNC(C[C@@H]1N=C(C2=CC(OC)=CC=C2N3C(C)=NN=C13)C4=CC=C(C=C4)Cl)=O
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.39 | 100 | |
| Ethanol | 42.39 | 100 |
Preparing Stock Solutions
for I-BET 762
The following data is based on the product molecular weight 423.90
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.36 mL | 11.80 mL | 23.59 mL |
| 5 mM | 0.47 mL | 2.36 mL | 4.72 mL |
| 10 mM | 0.24 mL | 1.18 mL | 2.36 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Mirguet Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. J.Med.Chem. 2013 PMID: 24015967
- Nicodeme Suppression of inflammation by a synthetic histone mimic. Nature 2010 PMID: 21068722
- Chaidos Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood 2014 PMID: 24335499
Product Specific Notices for I-BET 762
For research use only
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