AT13148 (C09-0735-487)

InformationAT13148 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.TargetsPKA (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 nMIn vitroAT13148, 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 vivoAT13148 (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. Specifications and Purity: 98%. Molecular Formula: C17H16ClN3O. Molecular Weight: 313.78. PubChem CID: 24905401. Isomeric SMILES: C1=CC(=CC=C1C2=CNN=C2)[C@@](CN)(C3=CC=C(C=C3)Cl)O. Related Document: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/A413783-SCI_1374748d739ccab626a5a5c70d171d29.pdf