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Vps34-IN-2
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Vps34-IN-2图片
CAS NO:1523404-29-6
规格:98%
分子量:402.41
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
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82nM。
CAS:1523404-29-6
分子式:C18H25F3N4O3
分子量:402.41
纯度:98%
存储:Store at -20°C

Background:

Vps34-IN-2 is a novel, potent and selective inhibitor of Vps34 with IC50s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively.


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)[1].


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[1].


[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. 2015 Jan 8;58(1):376-400.