I-BET 762

Pricing Availability   Qty
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)
Literature (4)

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
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
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.

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