M2698

M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC 50 s of 1 nM for p70S6K , Akt1 and Akt3 . M2698 can cross the blood-brain barrier and has anti-cancer activity In Vitro M2698 (0.3 nM to 50 M; 72 hours) inhibits proliferation in a dose-dependent manner in breast tumors cell lines with IC 50 s of 0.02-8.5 µM. 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. M2698 inhibits indirectly pGSK3β (IC 50 =17 nM) and pS6 (IC 50 =15 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Breast tumors cell lines Concentration: 0.3 nM to 50 M Incubation Time: 72 hours Result: Inhibited proliferation in a dose-dependent manner. Western Blot AnalysisCell Line: HCC1419 and MDA-MB-453 cells Concentration: 0.3, 1 µM Incubation Time: 24 hours Result: Inhibited p70S6K activity and induced feedback loop phosphorylation on Akt and suppressed Akt activity in breast cancer cell lines. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female nude mice bearing MDA-MB-468 tumors Dosage: 10, 20 and 30 mg/kg Administration: PO; daily; for 28 days Result: Resulted in dose-dependent inhibition of tumor growth and resulted in tumor regression with the highest dose of 30 mg/kg. Animal Model: Female SCID Beige mice with MDA-MB-453 xenografted Dosage: 20 mg/kg (Pharmacokinetic Analysis) Administration: Daily; for 4 days Result: Had a tumor:plasma exposure ratio of 12:1 over 24 hours. Form:Solid IC50& Target:p70S6K 1 nM (IC 50 ) Akt1 1 nM (IC 50 ) Akt3 1 nM (IC 50 )

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