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Glesatinib hydrochloride is an orally active and potent dual inhibitor of MET/SMO. Glesatinib hydrochloride is also a tyrosine kinase inhibitor. It antagonizes P-glycoprotein mediated multidrug resistance (MDR) in NSCLC.
Glesatinib hydrochloride is an orally active and potent dual inhibitor of MET/SMO. Glesatinib hydrochloride is also a tyrosine kinase inhibitor. It antagonizes P-glycoprotein mediated multidrug resistance (MDR) in NSCLC.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 9,540 | 6-8周 | |
50 mg | ¥ 12,400 | 6-8周 | |
100 mg | ¥ 17,400 | 6-8周 |
产品描述 | Glesatinib hydrochloride is an orally active and potent dual inhibitor of MET/SMO. Glesatinib hydrochloride is also a tyrosine kinase inhibitor. It antagonizes P-glycoprotein mediated multidrug resistance (MDR) in NSCLC. |
体外活性 | 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]. |
体内活性 | Glesatinib hydrochloride (15 mg/kg/day; orally; 40 weeks) results in an obvious reduction in tumor size [1]. |
别名 | MGCD265 hydrochloride |
分子量 | 656.16 |
分子式 | C31H28ClF2N5O3S2 |
CAS No. | 1123838-51-6 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | DMSO: 28 mg/mL (42.67 mM) | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
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