WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406200
CAS#: 22868-35-5
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.
MedKoo Cat#: 406200
Name: G-573
CAS#: 22868-35-5
Chemical Formula: C13H9ClN2
Exact Mass: 228.04543
Molecular Weight: 228.68
Elemental Analysis: C, 68.28; H, 3.97; Cl, 15.50; N, 12.25
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.
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
The following data is based on the product molecular weight 228.68 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Hatzivassiliou G, Haling JR, Chen H, Song K, Price S, Heald R, Hewitt JF, Zak M, Peck A, Orr C, Merchant M, Hoeflich KP, Chan J, Luoh SM, Anderson DJ, Ludlam MJ, Wiesmann C, Ultsch M, Friedman LS, Malek S, Belvin M. Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers. Nature. 2013 Sep 12;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, Zak M, Boggs J. Preclinical disposition and pharmacokinetics-pharmacodynamic modeling of biomarker response and tumour growth inhibition in xenograft mouse models of G-573, a MEK inhibitor. Xenobiotica. 2010 Nov;40(11):751-62. doi: 10.3109/00498254.2010.514365. PubMed PMID: 20836753.
