Glesatinib
Based on 2 publication(s) in Google Scholar
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).
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- CAS No.: 936694-12-1
- Formule: C31H27F2N5O3S2
- Masse moléculaire:619.70
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) Glesatinib
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KB 3-1 | IC50 |
0.004 μM
Compound: Glesatinib
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Antiproliferative activity against human KB-3-1 cells assessed as cell growth inhibition
Antiproliferative activity against human KB-3-1 cells assessed as cell growth inhibition
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[PMID: 38733884] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NSCLC H1299 cells
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Concentration:0.01, 0.1, 1, 2, 5 μM
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Incubation Time:For 72 hours
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Result:Resulted in a dose-dependent inhibition of cancer cell growth and showed the lowest IC50 value of 0.08 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4−6-week old female balb/c athymic (nu/nu) mice with HCC827 NSCLC tumor xenografts[1]
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Dosage:15 mg/kg
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Administration:Orally; daily; 40 weeks
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Result:Caused a significant decrease in tumor size.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 936694-12-1
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Masse moléculaire 619.70
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Formule C31H27F2N5O3S2
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SMILES
O=C(NC(NC1=CC=C(OC2=C3C(C=C(C4=NC=C(CNCCOC)C=C4)S3)=NC=C2)C(F)=C1)=S)CC5=CC=C(F)C=C5
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Synonyms
MGCD265
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Cell Rep
EGFR-phosphorylated GDH1 harmonizes with RSK2 to drive CREB activation and tumor metastasis in EGFR-activated lung cancer. [Abstract]2022 Dec 13;41(11):111827. PMID: 36516759
Pureté et documentation
Références
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Glesatinib Related Classifications
HY-19642 Related Classifications
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