[CAS NO. 1321924-70-2] VTX-27
PRODUCTS SPECIFICATIONS [1321924-70-2]
DESCRIPTION [1321924-70-2]
Overview
| MDL | MFCD31618412 |
|---|---|
| Molecular Weight | 418.90 |
| Molecular Formula | C20H24ClFN6O |
| SMILES | FC1=C(N=C(N2C[C@@](NCC2)([H])[C@](C)(O)C(C)C)C(Cl)=C1)C3=NNC4=NC=CC=C34 |
Summary
IC50 & Target
|
PKCθ 0.08 nM (Ki) |
PKCδ 16 nM (Ki) |
PKCα 356 nM (Ki) |
In Vitro
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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 C max concentration 700 ng/mL) and demonstrates potent dose dependent inhibition of IL-2 production [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 125 mg/mL ( 298.40 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3872 mL | 11.9360 mL | 23.8720 mL |
| 5 mM | 0.4774 mL | 2.3872 mL | 4.7744 mL |
| 10 mM | 0.2387 mL | 1.1936 mL | 2.3872 mL |
