Glesatinib  (Synonyms: MGCD265)

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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Glesatinib (MGCD265; 15 mg/kg/day; orally; 40 weeks) causes a significant decrease in tumor size^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

619.70

C₃₁H₂₇F₂N₅O₃S₂

936694-12-1

葛雷沙替尼

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]