I-BET 762

Key Product Details

Product Description

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.

Product Specifications for I-BET 762

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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.

Select a batch to recalculate based on the batch molecular weight:

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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

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 Documents for I-BET 762