Formulation: A solid
Formal Name: (αR,2S)-4-[3-chloro-5-fluoro-6-(1H-pyrazolo[3,4-b]pyridin-3-yl)-2-pyridinyl]-α-methyl-α-(1-methylethyl)-2-piperazinemethanol
Purity: ≥95%
Formula Markup: C20H24ClFN6O
Formula Weight: 418,9
Shelf life (days): 1460
CAS Number: 1321924-70-2
Notes: VTX-27 is a PKCθ inhibitor (Ki = 0.08 nM).{67037} It is selective for PKCθ over PKCα, -βI, -βII, -γ, -δ, -ε, -η, -µ, and -ζ with Ki values ranging from 1 to >5,000 nM as well as a panel of seven kinases from the Src, spleen tyrosine kinase (Syk), Tec, and MAP kinase families (Kis = >1,000 nM for all). VTX-27 inhibits CD28-induced IL-2 release in isolated human peripheral blood mononuclear cells (PBMCs; IC50 = 11 nM). Oral administration of VTX-27 (12.5, 25, and 50 mg/kg) prevents staphylococcal enterotoxin B-induced increases in IL-2 plasma levels in mice.
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