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Submit ReviewI-BET 762
Description: Potent and high affinity BET bromodomain inhibitor; anti-inflammatory; orally bioavailable.
Alternative Names: GSK525762A,Molibresib
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
Purity: ≥98% (HPLC)
Biological Activity for I-BET 762
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.
Technical Data for I-BET 762
| M. Wt | 423.9 |
| Formula | C22H22ClN5O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for I-BET 762
| 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 423.9. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.36 mL | 11.8 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 |
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Product Datasheets for I-BET 762
References for I-BET 762
References are publications that support the biological activity of the product.
Chaidos et al (2014) Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood 123 697 PMID: 24335499
Mirguet et al (2013) Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. J.Med.Chem. 56 7501 PMID: 24015967
Nicodeme et al (2010) Suppression of inflammation by a synthetic histone mimic. Nature 468 1119 PMID: 21068722
If you know of a relevant reference for I-BET 762, please let us know.
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Keywords: I-BET 762, I-BET 762 supplier, I-BET762, Potent, high, affinity, BRD, inhibitors, BET, bromodomains, anti-inflammatory, orally, bioavailable, BRD2, BRD3, BRD4, GSK525762A, Molibresib, Bromodomains, 6521, Tocris Bioscience
Citations for I-BET 762
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Literature in this Area
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