| Identification | Back Directory | [Name]
Glesatinib (hydrochloride) | [CAS]
1123838-51-6 | [Synonyms]
CS-2642
Glesatinib HCl
MGCD-265 HYDROCHLORIDE
Glesatinib (hydrochloride)
Glesatinib (hydrochloride)(MGCD265 hydrochloride) | [Molecular Formula]
C31H28ClF2N5O3S2 | [MDL Number]
MFCD30344661 | [MOL File]
1123838-51-6.mol | [Molecular Weight]
656.16 |
| Hazard Information | Back Directory | [Description]
Glesatinib HCl is a novel potent MET/SMO dual inhibitor. | [Uses]
Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC)[1][2]. | [in vivo]
Glesatinib hydrochloride (MGCD265 hydrochloride; 15 mg/kg/day; orally; 40 weeks) causes a significant decrease in tumor size[1].
| Animal Model: | 4?6-week old female balb/c athymic (nu/nu) mice with HCC827 NSCLC tumor xenografts[1] | | Dosage: | 15 mg/kg | | Administration: | Orally; daily; 40 weeks | | Result: | Caused a significant decrease in tumor size.
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| [References]
[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. DOI:10.1021/acs.jmedchem.7b00794
[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. DOI:10.3389/fonc.2019.00313 |
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