ChemicalBook--->CAS DataBase List--->936694-12-1

936694-12-1

936694-12-1 Structure

936694-12-1 Structure
IdentificationBack Directory
[Name]

Glesatinib
[CAS]

936694-12-1
[Synonyms]

Glesatinib
Glesatinib (MGCD-265
Benzeneacetamide, 4-fluoro-N-[[[3-fluoro-4-[[2-[5-[[(2-methoxyethyl)amino]methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxy]phenyl]amino]thioxomethyl]-
[Molecular Formula]

C31H27F2N5O3S2
[MDL Number]

MFCD30532644
[MOL File]

936694-12-1.mol
[Molecular Weight]

619.7
Chemical PropertiesBack Directory
[density ]

1.380±0.06 g/cm3(Predicted)
[pka]

9.47±0.70(Predicted)
Hazard InformationBack Directory
[Description]

Glesatinib is a TKI that targets tumors with MET and AXL alterations.
[Uses]

Glesatinib exhibits anti-tumor activity in lung cancer models and patients harboring MET exon 14 mutations and overcomes mutation-mediated resistance.
[Clinical Use]

Nonclinical models have shown glesatinib to be effective in MET exon 14 skipping mutations. It is currently being evaluated in phase II trials in NSCLC patients with MET alterations.
[in vivo]

Glesatinib (MGCD265; 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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