Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC). In Vitro Glesatinib hydrochloride (MGCD265 hydrochloride; 0.01-5 μM; for 72 hours) results in a dose-dependent inhibition of cancer cell growth and shows the low IC 50 value of 0.08 μM on NSCLC H1299 cells. Glesatinib hydrochloride (0.01, 0.1, 0.5, 1 μM) significantly increases by several-fold the percentage of apoptotic cells in 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 IC 50 s fell between 5 and 10 μM. Glesatinib hydrochloride (1, 3 μM; 120 mins) increases the intracellular [ 3 H]-Paclitaxel accumulation and inhibits [ 3 H]-Paclitaxel efflux in cancer cell lines overexpressing P-gp. Glesatinib hydrochloride (0-40 μM) stimulates the ATPase activity of P-gp transporters in a dose-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell 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 IC 50 value of 0.08 μM. In Vivo Glesatinib hydrochloride (MGCD265 hydrochloride; 15 mg/kg/day; orally; 40 weeks) causes a significant decrease in tumor size . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 4−6-week old female balb/c athymic (nu/nu) mice with HCC827 NSCLC tumor xenografts Dosage: 15 mg/kg Administration: Orally; daily; 40 weeks Result: Caused a significant decrease in tumor size. Form:Solid
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Glesatinib hydrochloride
CAS number：1123838-51-6 molecular formula：C31H28ClF2N5O3S2
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| Chinese alias | 盐酸格莱沙替尼 | ||
| English alias | - | ||
| CAS number | 1123838-51-6 | molecular formula | C31H28ClF2N5O3S2 |
| molecular weight | 656.17 g/mol | Exact mass | ≥98% |
| PSA | 158.000 Ų | logp | - |
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