Glesatinib
Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) [1][2].
Product Specifications
CAS Number
[936694-12-1]
Product Name Alternative
MGCD265
UNSPSC
12352005
Target
C-Met/HGFR; TAM Receptor
Type
Reference compound
Related Pathways
Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/glesatinib.html
Solubility
10 mM in DMSO
Smiles
O=C(NC(NC1=CC=C(OC2=C3C(C=C(C4=NC=C(CNCCOC)C=C4)S3)=NC=C2)C(F)=C1)=S)CC5=CC=C(F)C=C5
Molecular Formula
C31H27F2N5O3S2
Molecular Weight
619.70
References & Citations
[1]Morgillo F, et al. Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer. J Med Chem. 2017 Sep 14;60 (17) :7447-7458.|[2]Cui Q, et al. Glesatinib, a c-MET/SMO Dual Inhibitor, Antagonizes P-glycoprotein Mediated MultidrugResistance in Cancer Cells. Front Oncol. 2019 Apr 25;9:313.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 2
Citation 01
Cell Rep. 2022 Dec 13;41 (11) :111827.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.
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