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Glesatinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Glesatinib图片
CAS NO:936694-12-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
MGCD265
产品介绍
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.
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.
Clinical Trial
分子量

619.70

Formula

C31H27F2N5O3S2

CAS 号

936694-12-1

中文名称

葛雷沙替尼

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.