WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 201841
Description: MGCD265-analog, CAS#875337-44-3, is structurally related to MGCD-265 (Glesatinib). MGCD-265-analog is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity. MGCD-265-analog was introduced to the research community due to the wrong structure published in some database and publications. MGCD-265-analog has been sold as MGCD-265 by many reagent vendors since 2012. As of 4/28/2016, many drug-related database and suppliers still listed a wrong structure for MGCD-265. MGCD-265 (Glesatinib) has CAS#936694-12-1.
MedKoo Cat#: 201841
Chemical Formula: C26H20FN5O2S2
Exact Mass: 517.10424
Molecular Weight: 517.6
Elemental Analysis: C, 60.33; H, 3.89; F, 3.67; N,13.53; O, 6.18; S, 12.39
Synonym: MGCD-265-analog; MGCD 265-analog; MGCD265-analog. Glesatinib-analog.
IUPAC/Chemical Name: N-((3-fluoro-4-((2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)carbamothioyl)-2-phenylacetamide
SMILES Code: O=C(NC(NC1=CC=C(OC2=C3C(C=C(C4=CN(C)C=N4)S3)=NC=C2)C(F)=C1)=S)CC5=CC=CC=C5
MGCD265 is a novel targeted cancer therapeutic discovered by MethylGene that inhibits the Met and VEGF receptor tyrosine kinases. The abnormal activation of Met is involved in tumor development, metastasis and survival and the VEGF kinase is responsible for the inappropriate formation of blood vessels (angiogenesis) that nourish the tumor. In preclinical studies, MGCD265 demonstrated nanomolar potency in enzyme and cellular assays and up to 100% of tumor growth inhibition in a broad range of xenograft models.
Development Status of MGCD265: In the ongoing Phase 1 program, MGCD265 is being administered orally in patients with advanced cancers. The compound has demonstrated a favorable safety profile and can be combined safely with other cancer therapeutics such as docetaxel (TaxotereÂ®) and erlotinib (TarcevaÂ®). These therapeutics were selected for combination studies based on preclinical data that demonstrated the combination of MGCD265 and erlotinib and of MGCD265 and docetaxel showed greater anti-tumor activity compared to each drug administered alone. To date, the Company has initiated three clinical studies. (source: http://methylgene.com, accessed date: 2/1/2012)
J. M. Besterman, M. Fournel, I. Dupont, C. Bonfils, M. Dubay, H. Ste-Croix, C. R. Maroun; MethylGene, Inc., Montreal, QC, Canada, Potent preclinical antitumor activity of MGCD265, an oral Met/VEGFR kinase inhibitor in phase II clinical development, in combination with taxanes or erlotinib, J Clin Oncol 28, 2010 (suppl; abstr e13595).