Vps34-IN-2 is a potent and selective Vps34 inhibitor (IC50s: 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | 6-8 weeks | $ 192 | |
2 mg | 6-8 weeks | $ 364 | |
4 mg | 6-8 weeks | $ 517 | |
10 mg | 6-8 weeks | $ 1134 | |
20 mg | 6-8 weeks | $ 1814 |
Description | Vps34-IN-2 is a potent and selective Vps34 inhibitor (IC50s: 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively). |
Targets&IC50 | Vps34:2 nM |
In vitro | Vps34-IN-2 displays IC50s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively. Vps34-IN-2 exhibits selectivity against mTOR with IC50 more than 10 μM and class I PI3Ks with IC50 values of 2.7, 4.5, 2.5, and >10 μM on PI3K α, β, δ, γ isoforms, respectively. |
In vivo | After oral administration (po), Vps34-IN-2 is rapidly absorbed with maximal plasma concentrations observed at 0.5 h and a bioavailability of 85%. Slight rebounds of concentrations are observed at 4 and 8 h after oral dosing with no obvious explanation. After iv injection of Vps34-IN-2 at 3 mg/kg, plasma clearance is found moderate (i.e., 2.3 L/h/kg), corresponding to 44% of hepatic blood flow in this species, volume of distribution at steady state is moderate, and terminal elimination half-life is short. |
CAS No. | 1523404-29-6 |
Chemical Formula | C18H25F3N4O3 |
Molecular Weight | 402.418 |
Solubility | Ethanol: 50 mg/mL (124.25 mM), Need ultrasonic |
Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
bottom