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M2698
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。
M2698图片
CAS NO:1379545-95-5
包装:10 mg
市场价:8726元

产品名称
MSC2363318A
产品介绍

产品描述

M2698 can cross the blood-brain barrier and has anti-cancer activity. M2698 is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3.

体外活性

M2698 (0.3, 1 μM; 24 hours) inhibits p70S6K activity and induces feedback loop phosphorylation on Akt and suppresses Akt activity in breast cancer cell lines[1]. ?M2698 inhibits indirectly pGSK3β (IC50=17 nM) and pS6 (IC50=15 nM)[1].?M2698 (0.3 nM to 50 M;?72 hours) inhibits proliferation in a dose-dependent manner in breast tumors cell lines with IC50s of 0.02-8.5 μM[1].

体内活性

The mean total concentration of M2698 after 16-hour infusion in rats is 1750 ng/g and 175 ng/mL in brain and plasma, respectively[1]. ?M2698 (po; 1, 5, 10, or 20 mg/kg/day; for 7 days) inhibits the phosphorylation of S6 in a dose-proportional manner over time after a single administration or daily treatments over 7 days[1].?M2698 (10-30 mg/kg/day;?PO;?28 days) results in dose-dependent inhibition of tumor growth and results in tumor regression with the highest dose of 30 mg/kg[1].??M2698 (20 mg/kg/day;?PO;?4 days) has a tumor:plasma exposure ratio of 12:1 over 24 hours and leads to increased levels of pAkt in tumor tissue[1].

Cas No.

1379545-95-5

分子式

C21H19ClF3N5O

分子量

449.86

别名

MSC2363318A

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years