I-BET 762

Name: I-BET 762
Brand: Tocris Bioscience
SKU: 6521

Tocris Bioscience, part of Bio-Techne | Catalog # 6521

COA / SDS

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
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)
Molecular Weight:	423.9

View Full Technical Details for I-BET 762

Technical Data
Citations

Biological Activity for I-BET 762

I-BET 762 is a potent and high affinity BET bromodomain inhibitor (IC₅₀ = 32.5 - 42.5 nM; K_d = 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 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	11.80 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

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References for I-BET 762

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