Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: (aS)-a-(aminomethyl)-a-(4-chlorophenyl)-4-(1H-pyrazol-4-yl)-benzenemethanol
Purity: ≥98%
Formula Markup: C17H16ClN3O
Formula Weight: 313.8
CAS Number: 1056901-62-2
Notes: AT-13148 is an orally bioavailable and ATP-competitive multi-AGC kinase inhibitor.{38275} 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).{38276} Oral administration at a dose of 40 mg/kg reduces motility of 4699 melanoma cells in murine xenograft model.
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