Introduction：Basic information about CAS 936694-12-1|Glesatinib, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Glesatinib |
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| CAS Number | 936694-12-1 | Molecular Weight | 619.705 |
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| Density | 1.4±0.1 g/cm3 | Boiling Point | / |
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| Molecular Formula | C31H27F2N5O3S2 | Melting Point | / |
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| MSDS | / | Flash Point | / |
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Names
| Name | Glesatinib |
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| Synonym | More Synonyms |
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Glesatinib BiologicalActivity
| Description | 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]. |
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| Related Catalog | Research Areas >>CancerSignaling Pathways >>Protein Tyrosine Kinase/RTK >>TAM ReceptorSignaling Pathways >>Protein Tyrosine Kinase/RTK >>c-Met/HGFR |
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| Target | MET |
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| In Vitro | Glesatinib (MGCD265; 0.01-5 μM; for 72 hours) results in a dose-dependent inhibition of cancer cell growth and shows the low IC50 value of 0.08 μM on NSCLC H1299 cells[1]. Glesatinib (0.01, 0.1, 0.5, 1 μM) significantly increases by several-fold the percentage of apoptotic cells in NSCLC H1299 cells[1]. Glesatinib has the cytotoxicity to P-gp overexpressing cancer cells KB-C2, SW620/Ad300, HEK293/ABCB1, and their parent cells KB-3-1, SW620, HEK293 cells with the IC50s fell between 5 and 10 μM[1]. Glesatinib (1, 3 μM; 120 mins) increases the intracellular [3H]-Paclitaxel accumulation and inhibits [3H]-Paclitaxel efflux in cancer cell lines overexpressing P-gp[2]. Glesatinib (0-40 μM) stimulates the ATPase activity of P-gp transporters in a dose-dependent manner[2]. Cell Proliferation Assay[1] Cell Line: NSCLC H1299 cells Concentration: 0.01, 0.1, 1, 2, 5 μM Incubation Time: For 72 hours Result: Resulted in a dose-dependent inhibition of cancer cell growth and showed the lowest IC50 value of 0.08 μM. |
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| 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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| 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. [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. |
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Chemical & Physical Properties
| Density | 1.4±0.1 g/cm3 |
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| Molecular Formula | C31H27F2N5O3S2 |
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| Molecular Weight | 619.705 |
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| Exact Mass | 619.152344 |
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| LogP | 6.50 |
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| Index of Refraction | 1.672 |
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| InChIKey | YRCHYHRCBXNYNU-UHFFFAOYSA-N |
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| SMILES | COCCNCc1ccc(-c2cc3nccc(Oc4ccc(NC(=S)NC(=O)Cc5ccc(F)cc5)cc4F)c3s2)nc1 |
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Synonyms
| UNII:7Q29OXD98N |
| 7Q29OXD98N |
| N-[(3-Fluoro-4-{[2-(5-{[(2-methoxyethyl)amino]methyl}-2-pyridinyl)thieno[3,2-b]pyridin-7-yl]oxy}phenyl)carbamothioyl]-2-(4-fluorophenyl)acetamide |
| 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]- |
| Glesatinib |
