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MGCD265 dihydrochloride
- Glesatinib dihydrochloride - MG265 dihydrochloride
- Parent CAS: 936694-12-1
- Soluble in DMSO
- MF: C31H27F2N5O3S2.2HCl
- MW: 692.63
Description
MGCD265 is an orally bioavailable, multitargeted tyrosine kinase inhibitor. It 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). It is currently being evaluated clinically in patients with solid tumors that have genetic alterations in MET or AXL genes, which have been implicated as drivers of tumor growth and disease progression in NSCLC, gastroesophageal cancer and other solid tumors.
More Information
| Parent CAS No. | 936694-12-1 |
|---|---|
| Chemical Name | N-(3-Fluoro-4-(2-(5-((2-methoxyethylamino)methyl)pyridin-2-yl)thieno[3,2-b]pyridin-7-yloxy)phenylcarbamothioyl)-2-(4-fluorophenyl)acetamide |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1(OC2C=CN=C3C=C(C4N=CC(CNCCOC)=CC=4)SC=23)C=CC(NC(=S)NC(=O)CC2C=CC(F)=CC=2)=CC=1F.Cl.Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C31H27F2N5O3S2.2ClH/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);2*1H |
| InChiKey | KIMAMXOHRGHDBP-UHFFFAOYSA-N |
| CID | 25181472 |
| Short Description | MET/SMO dual inhibitor |
References
- F Morgillo 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.
- Q Cui et al. Glesatinib, a c-MET/SMO Dual Inhibitor, Antagonizes P-glycoprotein Mediated Multidrug Resistance in Cancer Cells. Front Oncol. 2019 Apr 25;9:313.
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