| Identification | Back Directory | [Name]
VTX-27 | [CAS]
1321924-70-2 | [Synonyms]
VTX-27
VTX-27 ≥95%
2-Piperazinemethanol, 4-[3-chloro-5-fluoro-6-(1H-pyrazolo[3,4-b]pyridin-3-yl)-2-pyridinyl]-α-methyl-α-(1-methylethyl)-, (αR,2S)- | [Molecular Formula]
C20H24ClFN6O | [MOL File]
1321924-70-2.mol | [Molecular Weight]
418.9 |
| Chemical Properties | Back Directory | [Boiling point ]
625.8±55.0 °C(Predicted) | [density ]
1.342±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: soluble | [form ]
A solid | [pka]
7.24±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
VTX-27 is a selective protein kinase C θ (PKC θ) inhibitor, with Kis of 0.08 nM and 16 nM for PKC θ and PKC δ. | [in vivo]
VTX-27 shows the best PK profile with a low clearance (7 mL min-1 kg-1), long half-life (4.7 h), and good oral bioavailability (65%). A single dose of VTX-27 is administered orally at 6.25, 12.5, 25, and 50 mg/kg (e.g., at 25 mg/kg Cmax concentration 700 ng/mL) and demonstrates potent dose dependent inhibition of IL-2 production[1]. | [IC 50]
PKCθ: 0.08 nM (Ki); PKCδ: 16 nM (Ki); PKCα: 356 nM (Ki) | [storage]
Store at -20°C | [References]
[1] Jimenez JM, et al. Design and optimization of selective protein kinase C θ (PKCθ) inhibitors for the treatment of autoimmune diseases. J Med Chem. 2013 Mar 14;56(5):1799-810. DOI:10.1021/jm301465a |
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Lynnchem
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Novachemistry
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https://www.novachemistry.com/ |
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