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AT-13148 is an orally bioavailable and ATP-competitive multi-AGC kinase inhibitor. It inhibits Akt1, 2, and 3 (IC50s = 38, 402, and 50 nM, respectively), in addition to other AGC kinase family members p70S6K, PKA, ROCK1, and ROCK2 (IC50s = 3-8 nM). AT-13148 inhibits growth of cancer cell lines with genetic mutations in PI3K-Akt-mTOR and RAS-RAF signaling pathways (GI50s = 1.54-3.77 µM). In vivo administration of AT-13148 (50 mg/kg, p.o.) inhibits the growth of MES-SA uterine sarcoma and BT474 breast cancer xenografts in mice by inhibiting Akt and p70S6K kinases. AT-13148 also stably inhibits ROCK-dependent phosphorylation of myosin light chain (MLC2) over a 24-hour period in 4599 mouse melanoma cells (EC50 = 0.1 µM). Oral administration at a dose of 40 mg/kg reduces motility of 4699 melanoma cells in murine xenograft model.Formal Name: (alphaS)-alpha-(aminomethyl)-alpha-(4-chlorophenyl)-4-(1H-pyrazol-4-yl)-benzenemethanol. CAS Number: 1056901-62-2. Molecular Formula: C17H16ClN3O. Formula Weight: 313.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml. lambdamax: 257 nm. SMILES: ClC1=CC=C([C@@](CN)(O)C2=CC=C(C3=CNN=C3)C=C2)C=C1. InChi Code: InChI=1S/C17H16ClN3O/c18-16-7-5-15(6-8-16)17(22,11-19)14-3-1-12(2-4-14)13-9-20-21-10-13/h1-10,22H,11,19H2,(H,20,21)/t17-/m0/s1. InChi Key: IIRWNGPLJQXWFJ-KRWDZBQOSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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