VTX-27 is a novel potent and selective PKCθ inhibitor.
CAS Number: 1321924-70-2
Molecular Weight: 418.90
Chemical Name: (2R)-2-[(2S)-4-[3-Chloro-5-fluoro-6-(2H-pyrazolo[3, 4-b]pyridin-3-yl)pyridin-2-yl]piperazin-2-yl]-3-methylbutan-2-ol
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
VTX-27 (Compound 27) possesses excellent overall characteristics. Good selectivity of VTX-27 is also seen against other PKC family members, particularly classical isoforms (>1000-fold except PKCβ I, 200-fold) and atypical isoforms (>10000-fold). As anticipated, attaining selectivity over the more closely related novel PKC family members is more challenging, with a good 200-fold being achieved over PKC δ.
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
- 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.
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