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

生物活性

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

化学信息

分子量	656.16
分子式	C₃₁H₂₈ClF₂N₅O₃S₂
CAS No.	1123838-51-6
Smiles	Cl.COCCNCc1ccc(nc1)-c1cc2nccc(Oc3ccc(NC(=S)NC(=O)Cc4ccc(F)cc4)cc3F)c2s1
密度	no data available

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 28 mg/mL (42.67 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (3.05 mM), Sonication is recommeded.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO