| Biochemical and Physiological Mechanisms | AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1. |
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| Product Description | Information AT13148 is an oral, ATP-competitive, multi-AGC kinaseinhibitor withIC50of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM forAkt1/2/3,p70S6K,PKA, andROCKI/II, respectively. Phase 1.
Targets PKA (Cell-free assay); ROCK2 (Cell-free assay); ROCK1 (Cell-free assay); p70S6K (Cell-free assay); Akt1 (Cell-free assay) 15565,3 nM; 4 nM; 6 nM; 8 nM; 38 nM
In vitro AT13148, as a multi-AGC kinase inhibitor, potently inhibits proliferation with GI50 values of 1.5 to 3.8 μM across a selected panel of cancer cell lines with deregulation of PI3K-AKT-mTOR or RAS-RAF pathways. In PTEN-deficient MES-SA cells, AT13148 also inhibits AKT and p70S6K signaling.
In vivo AT13148 (50 mg/kg p.o.) markedly inhibits the activity of both AKT and p70S6K AGC kinases, and subsequently exhibits marked antitumor effects in human tumor xenografts.
Cell Research(from reference) Cell lines：MES-SA, MES-SA/Dx5, BT474, HCT-116, A549, PC3, SK-BR-3, MCF7, U87MG, MDA-MB-468, DU-145, and SK-OV-3 cell lines Concentrations：~10 μM Incubation Time：72 hours or 96 hours |
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