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GSK 525762A

CAS No.
1260907-17-2
Chemical Name:
GSK 525762A
Synonyms
I-BET-762;GSK525762;Molibresib;GSK 525762A;IBET762(GSK525762A);Molibresib (I-BET762;GSK525762 (I-BET-762);GSK 525762A USP/EP/BP;GSK 525762A (I-BET-762);Molibresib (GSK 525762A)
CBNumber:
CB42627926
Molecular Formula:
C22H22ClN5O2
Molecular Weight:
423.9
MDL Number:
MFCD30207861
MOL File:
1260907-17-2.mol
Last updated:2023-06-30 15:45:59

GSK 525762A Properties

Melting point >132°C (dec.)
Density 1.35
storage temp. 2-8°C
solubility Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml)
form powder
pka 15.71±0.46(Predicted)
color white to beige
optical activity [α]/D +80 to +90°, c = 0.3 in methanol
Stability Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
FDA UNII 5QIO6SRZ2R

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P305+P351+P338
NFPA 704
0
3 0

GSK 525762A price More Price(34)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML1272 I-BET762 ≥98% (HPLC) 1260907-17-2 5MG $87.6 2024-03-01 Buy
Sigma-Aldrich SML1272 I-BET762 ≥98% (HPLC) 1260907-17-2 25MG $231.2 2024-03-01 Buy
Sigma-Aldrich 401010 I-BET - CAS 1260907-17-2 - Calbiochem 1260907-17-2 5MG $155 2024-03-01 Buy
Cayman Chemical 10676 I-BET762 ≥98% 1260907-17-2 1mg $32 2024-03-01 Buy
Cayman Chemical 10676 I-BET762 ≥98% 1260907-17-2 5mg $109 2024-03-01 Buy
Product number Packaging Price Buy
SML1272 5MG $87.6 Buy
SML1272 25MG $231.2 Buy
401010 5MG $155 Buy
10676 1mg $32 Buy
10676 5mg $109 Buy

GSK 525762A Chemical Properties,Uses,Production

Description

The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, affect inflammatory gene expression by controlling the assembly of histone acetylation-dependent chromatin complexes. I-BET762 is a synthetic compound which interacts with BET proteins with high-affinity (Kd = 32.5-42.5 nM). It blocks binding of BET proteins with acetylated histones, disrupting the formation of chromatin complexes involved in the expression of specific inflammatory genes in activated macrophages. Through these actions, I-BET762 provides protection against bacteria-induced sepsis and lipopolysaccharide-triggered endotoxic shock.

Uses

GSK 525762A, is a BET Bromodomain Inhibitor, which is now in clinical development. BET bromodomains have emerged as promising drug targets for treatment of cancers, inflammatory diseases, and other medical conditions.

Definition

ChEBI: 2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide is a benzodiazepine.

Biochem/physiol Actions

I-BET762 possesses anti-inflammatory property by controlling the pro-inflammatory gene expression. I-BET762 hinders the MYC (proto-oncogene) expression in cellular models. This action of I-BET762 might serve as an effective therapy in treating prostate cancer.

target

BET

storage

Store at -20°C

References

1) Nicodeme?et al.?(2010),?Suppression of inflammation by a synthetic histone mimic; Nature?468?1119 2) 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 3) Bandukwala?et al.?(2012),?Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors; Proc. Natl. Acad. Sci. USA,?109?14532 4) Delmore?et al.?(2011),?BET Bromodomain as a Therapeutic Strategy to Target c-Myc; Cell?146?904

GSK 525762A Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 135)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED
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Hubei Jusheng Technology Co.,Ltd.
18871490254 linda@hubeijusheng.com CHINA 28180 58
BOC Sciences
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Chongqing Chemdad Co., Ltd
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TargetMol Chemicals Inc.
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Career Henan Chemica Co
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HANGZHOU CLAP TECHNOLOGY CO.,LTD
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Dideu Industries Group Limited
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Finetech Industry Limited
+86-27-87465837 +8618971612321 info@finetechnology-ind.com China 9626 58
Zhejiang J&C Biological Technology Co.,Limited
+1-2135480471 +1-2135480471 sales@sarms4muscle.com China 10522 58

GSK 525762A Spectrum

I-BET-762 GSK 525762A (I-BET-762) GSK525762 (I-BET-762) GSK525762 4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, 6-(4-chlorophenyl)-N-ethyl-8-methoxy-1-methyl-, (4S)- (4S)-6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide GSK 525762A I-BET-762 GSK 525762A (4S)-6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide IBET762(GSK525762A) GSK 525762A (4S)-6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide (S)-2-(6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo-[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4 Molibresib (GSK 525762A) 2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide Molibresib Molibresib (GSK525762) (I-BET762) Molibresib (Synonyms: GSK 525762A GSK 525762A USP/EP/BP GSK525762A(Molibresib I-BET762) Molibresib (I-BET762 I-BET762 I-BET-762 GSK-525762A 2-((4S)-6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide I-BET762 (MOLIBRESIB) (GSK525762) GSK 525762A|||GSK525762|||I-BET 762 1260907-17-2 Inhibitors Apis