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M2698

CAS No. : 1379545-95-5

MCE 站：M2698

产品活性：M2698 (MSC2363318A) 是一种具有口服活性，ATP 竞争的，选择性的 p70S6K 和 Akt 双重抑制剂，对于 p70S6K，Akt1 和 Akt3 的 IC₅₀ 均为 1 nM。M2698 可以透过血脑屏障，具有抗癌活性。

研究领域：MAPK/ERK Pathway  |  PI3K/Akt/mTOR

作用靶点：Ribosomal S6 Kinase (RSK)  |  Akt

In Vitro: 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 ?M.
M2698 (0.3, 1 ?M; 24 hours) inhibits p70S6K activity and induces feedback loop phosphorylation on Akt and suppresses Akt activity in breast cancer cell lines.
M2698 inhibits indirectly pGSK3β (IC₅₀=17 nM) and pS6 (IC₅₀=15 nM).

In Vivo: 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.
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.
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.
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.

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