S82022 |
Glesatinib (hydrochloride) |
| 源叶(MedMol) | 98% |
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- 产品描述： 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)
- 靶点： TAM Receptor;c-Met/HGFR
- 体外研究： 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 IC50 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 IC50s fell between 5 and 10 μM. Glesatinib hydrochloride (1, 3 μM; 120 mins) increases the intracellular [3H]-Paclitaxel accumulation and inhibits [3H]-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. Cell Proliferation Assay Cell 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 IC50 value of 0.08 μM.
- 体内研究： Glesatinib hydrochloride (MGCD265 hydrochloride; 15 mg/kg/day; orally; 40 weeks) causes a significant decrease in tumor size. 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.
- 参考文献：
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.
- 溶解性： soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 1.526 ml 7.632 ml 15.264 ml 5 mM 0.305 ml 1.526 ml 3.053 ml 10 mM 0.153 ml 0.763 ml 1.526 ml 50 mM 0.031 ml 0.153 ml 0.305 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
