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Cat #: V32664 CAS #: 1523404-29-6 Purity ≥ 99%
Description: Vps34-IN-2 is a novel and potent inhibitor of Vps34 (IC50s = 2 and 82 nM for enzymatic and cellular assay, respectively). Reference: 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
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Molecular Weight (MW) | 402.41 |
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Molecular Formula | C₁₈H₂₅F₃N₄O₃ |
CAS No. | 1523404-29-6 |
Protocol | In Vitro | 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]. |
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In Vivo | 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]. |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.4850 mL | 12.4251 mL | 24.8503 mL | 49.7006 mL |
5mM | 0.4970 mL | 2.4850 mL | 4.9701 mL | 9.9401 mL |
10mM | 0.2485 mL | 1.2425 mL | 2.4850 mL | 4.9701 mL |
20mM | 0.1243 mL | 0.6213 mL | 1.2425 mL | 2.4850 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.