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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
PI4KIIIβ-IN-10 (PI4KIIIbeta-IN-10) is a novel, potent and selective PI4KIIIβ (Type III phosphatidylinositol 4-kinase) inhibitor with an IC50 of 3.6 nM with >1000-fold over class I and class III PI3Ks. Type III phosphatidylinositol 4-kinase (PI4KIIIβ) is an essential enzyme in mediating membrane trafficking and is implicated in a variety of pathogenic processes. It is a crucial host factor that facilitates the replication of RNA viruses. The development of effective and targeted inhibitors of this enzyme will be crucial for defining its cellular functions and could result in brand-new antiviral therapeutics. Hepatitis C virus infection was inhibited by PI4KIIIβ-IN-9.
| Targets |
PI4KIIIβ (IC50 = 3.6 nM); PI4KIIIα (IC50 = 3 μM); PI3Kδ (IC50 = 720 nM); PI3KC2γ (IC50 = 1 μM); PI3Kα (IC50 = 10 μM); PI3Kγ (IC50 = 20 μM)
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|---|---|
| ln Vitro |
PI4KIIIbeta-IN-10 (Compound 10) is a potent PI4KIIIβ inhibitor with very minor off-target inhibition of PI4KIIIβ related lipid kinases. PI4KIIIbeta-IN-10 exhibits weak inhibition of PI3KC2γ (IC50 ~1 µM), PI3Kα (~10 µM), and PI4KIIIα (~3 µM), and <20% inhibition of PI4K2α, PI4K2β, and PI3Kβ at concentrations up to 20 µM[1].
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| Enzyme Assay |
Lipid kinase assays are preformed using recombinant enzyme, phosphoinositides and γ32P-ATP in a membrane capture assay. Every inhibitor (for instance, PI4KIIIbeta-IN-10) is diluted with 10% DMSO and kinase assay buffer. As soon as the reaction is finished, 4 µL is spotted onto nitrocellulose with a 0.2 µm thickness. After drying for 5 minutes under a heat lamp, the membrane is washed in 1M NaCl/1% Phosphoric Acid for 1 minute, then 6 times for 5 minutes. The membrane is dried for 20 minutes using a heat lamp, then exposed to a phosphor screen overnight, followed by phosphorimaging on a Typhoon 9500. SPOT is used to measure intensity. Following are the details for each enzyme. To create 1 mg/mL PI:, L--phosphotidylinositol and DOPS:DOPC lipids are sonicated in water. DOPS:DOPC. Reaction is set-up as follows 1) kinase assay buffer, PI:DOPS:DOPC, BSA and PI4KIIIβ, are combined in a total volume of 10 µL (2.5x solution); 2) 5 µL of inhibitor solution is added (5x solution) and incubated with enzyme mixture for 15 minutes; 3) 10 µL cold ATP and γ32P-ATP are added (2.5x solution) to initiate the reaction which ran for 30 minutes. Final conditions are as follows: 20 mM Bis-Tris Propane pH 7.5, 10 mM MgCl2, 0.075 mM Triton X-100, 0.5 mM EGTA, 1 mM DTT, 100 µM PI, 500 ng/µL BSA, 2.5 nM PI4KIIIβ, 2% DMSO, 10 µM ATP and 1 uCi γ32P-ATP[1].
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| References |
| Molecular Formula |
C22H25N3O5S2
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|---|---|
| Molecular Weight |
475.5810
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| Exact Mass |
475.123
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| Elemental Analysis |
C, 55.56; H, 5.30; N, 8.84; O, 16.82; S, 13.48
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| CAS # |
1881233-39-1
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| Related CAS # |
1881233-39-1; 1429624-84-9 (PI4KIIIβ-IN-9); 1429624-84-9 (PI4KIIIβ-IN-9)
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| PubChem CID |
71549093
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.631
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| LogP |
3.64
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
32
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| Complexity |
744
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1=C(C([H])=C([H])C(=C1[H])C1=C(C([H])([H])[H])N=C(N([H])C(C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])=O)S1)OC([H])([H])[H])(N([H])C1C([H])=C([H])C(=C([H])C=1[H])O[H])(=O)=O
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| InChi Key |
PLUYFBRIGUAKBR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H25N3O5S2/c1-13-19(31-21(23-13)24-20(27)22(2,3)4)14-6-11-17(30-5)18(12-14)32(28,29)25-15-7-9-16(26)10-8-15/h6-12,25-26H,1-5H3,(H,23,24,27)
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| Chemical Name |
N-[5-[3-[(4-hydroxyphenyl)sulfamoyl]-4-methoxyphenyl]-4-methyl-1,3-thiazol-2-yl]-2,2-dimethylpropanamide
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| Synonyms |
PI4KIIIβ-IN-10; PI4KIIIbeta-IN-10; PI4KIIIβ-IN 10; PI4KIIIbeta-IN 10; PI4KIIIβ-IN10; PI4KIIIbeta-IN10
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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: ~125 mg/mL (~262.8 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.26 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 (5.26 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 (5.26 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 | 2.1027 mL | 10.5135 mL | 21.0270 mL | |
| 5 mM | 0.4205 mL | 2.1027 mL | 4.2054 mL | |
| 10 mM | 0.2103 mL | 1.0513 mL | 2.1027 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.
Activity of AZD8186. Mol Cancer Ther. 2015, 14(1), 48-58. |
In vivo activity of AZD8186 |
AZD8186 combines with docetaxel. |
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