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VPS34-IN1 (VPS34-IN-1) is a novel and potent Vps34 (vacuolar protein sorting 34) inhibitor with potential antitumor activity. It has an IC50 of 25 nM for Vps34 inhibition and no activity for 350 closely related lipid or protein kinases. Phosphorylation of PtdIns (phosphatidylinositol) at endosomal membranes by the Vps34 class III PI3K results in PtdIns(3)P, which controls membrane trafficking processes by attracting a subset of proteins with PtdIns(3)P-binding PX (phox homology) and FYVE domains.
Targets |
Vps34 (IC50 = 4 nM)
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ln Vitro |
Administration of VPS34-IN1 to cells induces a rapid dose-dependent dispersal of a specific PtdIns(3)P-binding probe from endosome membranes, within 1min, without affecting the ability of class I PI3K to regulate Akt. Additionally, it has the ability to quickly reduce SGK3 phosphorylation by between 50 and 60 percent in just one minute. When it comes to SGK2 isoforms lacking a PtdIns(3)P-binding PX domain, VPS34-IN1 has no inhibitory effect[1].
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References |
Molecular Formula |
C21H24CLN7O
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Molecular Weight |
425.9146
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Exact Mass |
425.17309
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Elemental Analysis |
C, 59.22; H, 5.68; Cl, 8.32; N, 23.02; O, 3.76
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CAS # |
1383716-33-3
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Related CAS # |
1383716-33-3
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Appearance |
White to off-white Solid powder
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SMILES |
CC(C)(CNC1=NC=C(C(=N1)CC2CC2)C3=NC(=NC=C3)NC4=CC(=NC=C4)Cl)O
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InChi Key |
AWNXKZVIZARMME-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C21H24ClN7O/c1-21(2,30)12-26-19-25-11-15(17(29-19)9-13-3-4-13)16-6-8-24-20(28-16)27-14-5-7-23-18(22)10-14/h5-8,10-11,13,30H,3-4,9,12H2,1-2H3,(H,25,26,29)(H,23,24,27,28)
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Chemical Name |
1-[[5-[2-[(2-chloropyridin-4-yl)amino]pyrimidin-4-yl]-4-(cyclopropylmethyl)pyrimidin-2-yl]amino]-2-methylpropan-2-ol
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Synonyms |
VPS34IN1; VPS34-IN1; VPS34 IN1
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~85 mg/mL (~199.6 mM)
Ethanol: ~85 mg/mL (~199.6 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.87 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.87 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3479 mL | 11.7396 mL | 23.4791 mL | |
5 mM | 0.4696 mL | 2.3479 mL | 4.6958 mL | |
10 mM | 0.2348 mL | 1.1740 mL | 2.3479 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(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.
VPS34-IN1 reduces GFP–2×FYVEHrs probe localization on endosomes in a dose-dependent manner. Biochem J . 2014 Nov 1;463(3):413-27. td> |
VPS34-IN1 reduces GFP–2×FYVEHrs probe localization on endosomes in a dose-dependent manner. Biochem J . 2014 Nov 1;463(3):413-27. td> |