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| 5mg |
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| 10mg |
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| 25mg |
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Centrinone (LCR263; LCR-263; LCR 263) is a novel and potent inhibitor of polo-like kinase 4 (PLK4) with potential antineoplastic activity. It exhibits >1000-fold selectivity for PLK4 over Aurora A and Aurora B and inhibits PLK4 with a Ki of 0.16 nM.
| Targets |
PLK4 (Ki = 0.16 nM); PLK4 (G95L) (Ki = 68.57 nM); Aurora A (Ki = 171 nM); Aurora B (Ki = 436.76 nM)
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| ln Vitro |
Centrinone (LCR-263) inhibits Plk4 to stop centriole assembly.In human and other vertebrate cells, centrinone treatment results in centrosome depletion.
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| Enzyme Assay |
The human Plk4 kinase domain with 6xHis tag has been purified and is stored in 20 mM Tris pH 7.5, 100 mM NaCl, 10% glycerol, and 1 mM DTT. The contents of the 2X reaction buffer are as follows: 50 mM HEPES pH 8.5, 20 mM MgCl2, 1 mM DTT, 0.2 mg/mL BSA, 16 μM ATP, and 200 μM A-A11 substrate. At a pH of 8.0, the final reaction contains 2.5–10 nM of Plk4. DMSO stocks are used to add inhibitors (Centrinone) that vary in dose response. Reactions are permitted to continue at 25°C for 4–16 hours. ADP-Glo reagent is used for detection. Plate readers are used to measure luminosity.
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| Cell Assay |
Cells are seeded at 50,000 cells/well in triplicate into 6-well plates for each condition. HeLa cells receive 125 nM Centrinone (LCR-263) addition, while NIH/3T3 cells receive 300 nM. Three wells are harvested for each condition every twenty-four hours. An automated cell counter called the TC10 is used to count cells.
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| References |
| Molecular Formula |
C26H25F2N7O6S2
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|---|---|
| Molecular Weight |
633.65
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| Exact Mass |
633.12758
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| Elemental Analysis |
C, 49.28; H, 3.98; F, 6.00; N, 15.47; O, 15.15; S, 10.12
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| CAS # |
1798871-30-3
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| Related CAS # |
Centrinone-B;1798871-31-4
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| Appearance |
Solid powder
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| SMILES |
CC1=CC(=NN1)NC2=C(C(=NC(=N2)SC3=C(C=C(C=C3)S(=O)(=O)CC4=C(C(=CC=C4)[N+](=O)[O-])F)F)N5CCOCC5)OC
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| InChi Key |
HHJSKDRCUMVWKF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H25F2N7O6S2/c1-15-12-21(33-32-15)29-24-23(40-2)25(34-8-10-41-11-9-34)31-26(30-24)42-20-7-6-17(13-18(20)27)43(38,39)14-16-4-3-5-19(22(16)28)35(36)37/h3-7,12-13H,8-11,14H2,1-2H3,(H2,29,30,31,32,33)
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| Chemical Name |
2-[2-fluoro-4-[(2-fluoro-3-nitrophenyl)methylsulfonyl]phenyl]sulfanyl-5-methoxy-N-(5-methyl-1H-pyrazol-3-yl)-6-morpholin-4-ylpyrimidin-4-amine
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| Synonyms |
LCR263; LCR 263; LCR-263; Centrinone
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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: ≥ 31 mg/mL (~48.9 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.95 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 (3.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5782 mL | 7.8908 mL | 15.7816 mL | |
| 5 mM | 0.3156 mL | 1.5782 mL | 3.1563 mL | |
| 10 mM | 0.1578 mL | 0.7891 mL | 1.5782 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.
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