G-573

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WARNING: This product is for research use only, not for human or veterinary use.

Description:G-573 is an allosteric inhibitor of MEK that is both potent and selective. The IC(50) value for pERK inhibition in HCT116 tumours by G-573 was estimated to be 0.406  µM. The IC(50) values for tumour growth inhibition in HCT116 and H2122 were estimated to be 3.43 and 2.56 µM, respectively. ED(50) estimates in HCT116 and H2122 mouse xenograft models were estimated to be ~4.6 and 1.9 mg/kg/day, respectively.

Price and Availability

G-573, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 406200Name: G-573CAS#: 22868-35-5Chemical Formula: C13H9ClN2Exact Mass: 228.04543Molecular Weight: 228.68Elemental Analysis: C, 68.28; H, 3.97; Cl, 15.50; N, 12.25

Synonym:G573; G-573; G 573.

IUPAC/Chemical Name:2-(3-chlorophenyl)-1H-benzo[d]imidazole

InChi Key:BGYHTIIVIGGCIF-UHFFFAOYSA-N

InChi Code:InChI=1S/C13H9ClN2/c14-10-5-3-4-9(8-10)13-15-11-6-1-2-7-12(11)16-13/h1-8H,(H,15,16)

SMILES Code:ClC1=CC(C2=NC3=CC=CC=C3N2)=CC=C1

Technical Data

Additional Information

References

1: Hatzivassiliou G, Haling JR, Chen H, Song K, PriceS, Heald R, Hewitt JF, Zak  M, Peck A, Orr C, Merchant M, HoeflichKP, Chan J, Luoh SM, Anderson DJ, Ludlam MJ, Wiesmann C, Ultsch M,Friedman LS, Malek S, Belvin M. Mechanism of MEK inhibition determinesefficacy in mutant KRAS- versus BRAF-driven cancers. Nature. 2013 Sep12;501(7466):232-6. doi: 10.1038/nature12441. Epub 2013 Aug 11. Erratum in: Nature. 2013 Oct 10;502(7470):258. PubMed PMID: 23934108.

2: Choo EF, Belvin M, Chan J, Hoeflich K, Orr C, Robarge K, Yang X, ZakM, Boggs  J. Preclinical disposition and pharmacokinetics-pharmacodynamicmodeling of biomarker response and tumour growth inhibition in xenograftmouse models of G-573, a MEK inhibitor. Xenobiotica. 2010Nov;40(11):751-62. doi: 10.3109/00498254.2010.514365. PubMed PMID:20836753.