[CAS NO. 726695-51-8] SykInhibitorII
PRODUCTS SPECIFICATIONS [726695-51-8]
DESCRIPTION [726695-51-8]
Overview
| MDL | MFCD12922523 |
|---|---|
| Molecular Weight | 340.30 |
| Molecular Formula | C14H15F3N6O |
| SMILES | O=C(C1=CN=C(NCCN)N=C1NC2=CC=CC(C(F)(F)F)=C2)N |
Summary
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC 50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC 50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect [1] .
IC50 & Target
|
Syk 41 nM (IC 50 ) |
serotonin 460 nM (IC 50 ) |
PKCε 5.1 μM (IC 50 ) |
PKCβ2 11 μM (IC 50 ) |
ZAP-70 11.2 μM (IC 50 ) |
Btk 15.5 μM (IC 50 ) |
Itk 22.6 μM (IC 50 ) |
In Vitro
Syk Inhibitor II (compound 9a) shows less potent against PKCε, PKCβ2, ZAP-70, Btk, and Itk with IC 50 values of 5.1 µM, 11 µM, 11.2 µM, 15.5 µM, and 22.6 µM, respectively [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Syk Inhibitor II (Compound 9a; 10-100 mg/kg) is subcutaneously administered to mice 30 min before antigen challenge. Syk Inhibitor II inhibits the anaphylaxis reaction dose-dependently with an ID 50 value of 13.2 mg/kg [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 : 5 mg/mL ( 14.69 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9386 mL | 14.6929 mL | 29.3858 mL |
| 5 mM | 0.5877 mL | 2.9386 mL | 5.8772 mL |
| 10 mM | 0.2939 mL | 1.4693 mL | 2.9386 mL |
