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Glesatinib

Catalog No. T15384   CAS 936694-12-1
Synonyms: MGCD265

Glesatinib is an orally active and potent dual inhibitor of MET/SMO. Glesatinib is also a tyrosine kinase inhibitor. It antagonizes P-glycoprotein mediated multidrug resistance (MDR) in NSCLC.

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Glesatinib Chemical Structure
Glesatinib, CAS 936694-12-1
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,670.00
50 mg 6-8 weeks $ 2,180.00
100 mg 6-8 weeks $ 2,800.00
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Glesatinib is an orally active and potent dual inhibitor of MET/SMO. Glesatinib is also a tyrosine kinase inhibitor. It antagonizes P-glycoprotein mediated multidrug resistance (MDR) in NSCLC.
In vitro Glesatinib hydrochloride (0.01, 0.1, 0.5, 1 μM) obviously enhances by several-fold the percentage of apoptotic cells in NSCLC H1299 cells. Glesatinib hydrochloride (0.01-5 μM; for 72 hours) causes a dose-dependent inhibition of cancer cell growth (IC50: 0.08 μM on NSCLC H1299 cells). Glesatinib hydrochloride 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 hydrochloride (0-40 μM) stimulates the ATPase activity of P-gp transporters in a dose-dependent manner. Glesatinib hydrochloride (1, 3 μM; 120 mins) enhances the intracellular [3H]-Paclitaxel accumulation and inhibits [3H]-Paclitaxel efflux in cancer cell lines overexpressing P-gp [2].
In vivo Glesatinib hydrochloride (15 mg/kg/day; orally; 40 weeks) results in an obvious reduction in tumor size [1].
Synonyms MGCD265
Molecular Weight 619.7
Formula C31H27F2N5O3S2
CAS No. 936694-12-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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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Keywords

Glesatinib 936694-12-1 Tyrosine Kinase/Adaptors c-Met/HGFR MGCD-265 MGCD265 MGCD 265 inhibitor inhibit

 

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