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Glesatinib hydrochloride
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 hydrochloride图片
CAS NO:1123838-51-6
包装与价格:
包装价格(元)
25 mg电议
50 mg电议
100 mg电议

产品名称
MGCD265 hydrochloride
产品介绍

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].

Cas No.

1123838-51-6

分子式

C31H28ClF2N5O3S2

分子量

656.16

别名

MGCD265 hydrochloride

储存和溶解度

DMSO:28 mg/mL (42.67 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years