Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Glesatinib 936694-12-1 Tyrosine Kinase/Adaptors c-Met/HGFR MGCD-265 MGCD265 MGCD 265 inhibitor inhibit