Vps34-IN-2 是一种新型的，有效且有选择性的 Vps34 抑制剂，在 Vps34 酶促测定和 GFP-FYVE 细胞测定中的 IC₅₀ 值分别为 2 和 82 nM。Vps34-IN-2 对 SARS-CoV-2 (IC₅₀ 为 3.1 μM)，HCoV-229E (IC₅₀ 为 0.7 μM) 和 HCoV-OC43 具有抗病毒活性。

Vps34-IN-2 is a novel, potent and selective inhibitor of Vps34 with IC 50 s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively. Vps34-IN-2 shows antiviral activity against SARS-CoV-2 (IC 50 of 3.1 μM), HCoV-229E (IC 50 of 0.7 μM) and HCoV-OC43.

Solid

Vps34 2 nM (IC50) SARS-CoV-2 3.1 μM (IC

Vps34-IN-2 (Compound 31) 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 (IC50>10 μM) and class I PI3Ks (IC50 values of 2.7, 4.5, 2.5, and >10 μM on PI3K α, β, δ, γ isoforms, respectively). has not independently confirmed the accuracy of these methods. They are for reference only.

After administration by the intravenous (iv) route, Vps34-IN-2 (Compound 31) concentrations are quantifiable up to 6, 8, and 24 h (last sampling time) depending on animals. 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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Pasquier B, et al. Discovery of (2S)-8-[(3R)-3-methylmorpholin-4-yl]-1-(3-methyl-2-oxobutyl)-2-(trifluoromethyl)-3,4-dihydro-2H-pyrimido[1,2-a]pyrimidin-6-one: a novel potent and selective inhibitor of Vps34 for the treatment of solid tumors. J Med Chem.
[2]. Jim Baggen, et al. Genome-wide CRISPR screening identifies TMEM106B as a proviral host factor for SARS-CoV-2. Nat Genet. 2021 Mar 8.

In Vitro: Ethanol : 50 mg/mL (124.25 mM; Need ultrasonic)配制储备液