A dual inhibitor of p70S6K and Akt1
M2698 is a dual inhibitor of p70 ribosomal S6 kinase (p70S6K) and Akt1 (IC50s = 1.1 and 4 nM, respectively).1 It is selective for p70S6K and Akt1 over Aurora B kinase (IC50 = 170 nM), as well as a panel of 265 kinases at 1 ?M, but also inhibits protein kinase A (PKA), p90 ribosomal S6 kinase 1 (MSK1), MSK2, cGMP-dependent protein kinase 1α (PKG1α), PKG1β, and protein kinase X (PRKX). M2698 reduces tumor volume in MiaPaCa-2 pancreatic cancer and A549 non-small cell lung cancer (NSCLC) mouse xenograft models when administered at doses of 20 or 30 mg/kg, respectively.
1.DeSelm, L., Huck, B., Lan, R., et al.Identification of clinical candidate M2698, a dual p70S6K and Akt inhibitor, for treatment of PAM pathway-altered cancersJ. Med. Chem.64(19)14603-14619(2021)
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