I-BET762 (GSK525762) --- BET Inhibitor


Catalog No. size PriceQuantity
M60154-2D 10 mM in DMSO (0.472 mL) $139
M60154-2S 2mg solid $139
M60154-10S 10 mg solid $570

Description

I-BET762 (GSK525762) is a novel, highly potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~35 nM. It suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation. It is highly selective over other bromodomain-containing proteins. In vivo studies using I-BET762 have demonstrated efficacy in a range of oncology and immunoinflammatory models. I-BET762 is currently in clinical development for oncology indication.

Product information

CAS Number: 1260907-17-2

Molecular Weight: 423.90

Formula: C22H22ClN5O2

Synonym:

GSK525762

Chemical Name: (S)-2-(6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide

Smiles: CC1=NN=C2[C@H](CC(=O)NCC)N=C(C3=CC(=CC=C3N12)OC)C1C=CC(Cl)=CC=1

InChiKey: AAAQFGUYHFJNHI-SFHVURJKSA-N

InChi: InChI=1S/C22H22ClN5O2/c1-4-24-20(29)12-18-22-27-26-13(2)28(22)19-10-9-16(30-3)11-17(19)21(25-18)14-5-7-15(23)8-6-14/h5-11,18H,4,12H2,1-3H3,(H,24,29)/t18-/m0/s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 50 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

I-BET762 was used at 0.5-1 µM final concentration in various in vitro assays.

In Vivo:

I-BET762 could be dosed to the mice by oral administration at 10-30 mg/kg once per day.

References:

  1. Mirguet O, et al. Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. (2013) J Med Chem. 56(19):7501-15.
  2. Zhao Y, et al. The making of I-BET762, a BET bromodomain inhibitor now in clinical development. (2013) J Med Chem. 56(19):7498-500.

Products are for research use only. Not for human use.


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