Glesatinib (MGCD265) 是一种具有口服活性的，有效的MET/SMO双抑制剂。 Glesatinib 是一种酪氨酸激酶抑制剂，可拮抗非小细胞肺癌 (NSCLC) 中 P 糖蛋白介导的多药耐药性 (MDR)。
| 生物活性 | Glesatinib (MGCD265) is an orally active, potentMET/SMOdual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizesP-glycoprotein(P-gp) mediated multidrug resistance (MDR) in non-small cell lungcancer(NSCLC)[1][2]. |
体外研究
(In Vitro) | Glesatinib (MGCD265; 0.01-5 μM; for 72 hours) results in a dose-dependent inhibition of cancer cell growth and shows the low IC50value 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].
Cell Proliferation Assay[1] | 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 IC50value of 0.08 μM. |
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体内研究
(In Vivo) | Glesatinib (MGCD265; 15 mg/kg/day; orally; 40 weeks) causes a significant decrease in tumor size[1].
| Animal Model: | 4–6-week old female balb/c athymic (nu/nu) mice with HCC827 NSCLC tumor xenografts[1] | | Dosage: | 15 mg/kg | | Administration: | Orally; daily; 40 weeks | | Result: | Caused a significant decrease in tumor size. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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