Glesatinib (MGCD-265)

• CAT Number: I006613
• CAS Number: 936694-12-1
• Molecular Formula: C31H27F2N5O3S2
• Molecular Weight: 619.7
• Purity: ≥95%
• Target: TKI inhibitor
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4°C for short term or -20 °C for long term
• IUPAC Name: N-[[3-fluoro-4-[2-[5-[(2-methoxyethylamino)methyl]pyridin-2-yl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]carbamothioyl]-2-(4-fluorophenyl)acetamide
• InChI: InChI=1S/C31H27F2N5O3S2/c1-40-13-12-34-17-20-4-8-24(36-18-20)28-16-25-30(43-28)27(10-11-35-25)41-26-9-7-22(15-23(26)33)37-31(42)38-29(39)14-19-2-5-21(32)6-3-19/h2-11,15-16,18,34H,12-14,17H2,1H3,(H2,37,38,39,42)
• InChIKey: YRCHYHRCBXNYNU-UHFFFAOYSA-N
• SMILES: COCCNCC1=CN=C(C=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=S)NC(=O)CC5=CC=C(C=C5)F)F

Glesatinib (Cat.No:I006613), also known as MGCD-265, is an orally bioavailable, small-molecule, multitargeted tyrosine kinase inhibitor with potential antineoplastic activity. MGCD265 binds to and inhibits the phosphorylation of several receptor tyrosine kinases (RTKs), including the c-Met receptor (hepatocyte growth factor receptor); the Tek/Tie-2 receptor; vascular endothelial growth factor receptor (VEGFR) types 1, 2, and 3; and the macrophage-stimulating 1 receptor (MST1R or RON).

Reference

1:Padda S, Neal JW, Wakelee HA. MET inhibitors in combination with other therapies in non-small cell lung cancer. Transl Lung Cancer Res. 2012 Dec;1(4):238-53. doi: 10.3978/j.issn.2218-6751.2012.10.08. Review. PubMed PMID: 25806189; PubMed Central PMCID: PMC4367550.2:Belalcazar A, Azaña D, Perez CA, Raez LE, Santos ES. Targeting the Met pathway in lung cancer. Expert Rev Anticancer Ther. 2012 Apr;12(4):519-28. doi: 10.1586/era.12.16. Review. PubMed PMID: 22500688.