ChemicalBook--->CAS DataBase List--->1123838-51-6

1123838-51-6

1123838-51-6 Structure

1123838-51-6 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

DMSO : ≥ 28 mg/mL (42.67 mM)
[form ]

Solid
[color ]

Off-white to pink
Hazard InformationBack 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.
[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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