M2698

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity.

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 Analysis Cell 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.

Animal Model:Female nude mice bearing MDA-MB-468 tumorsDosage: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.

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Cytoskeleton/Cell Adhesion Molecules

Akt

Akt | mTOR

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1379545-95-5

449.86

C21H19ClF3N5O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 125 mg/mL (277.86 mM; 超声助溶 )

N([C@H](CN1CCC1)C2=CC(C(F)(F)F)=C(Cl)C=C2)C=3C4=C(C(C(N)=O)=CC=C4)N=CN3

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(-20℃)

With Ice Pack

≥ 2 years