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Purity: ≥98%
RGFP966 (RGF-P966) is a novel, potent and highly selective inhibitor of HDAC3 (histone deacetylase 3) with potential anticancer activity. In a cell-free assay, it inhibits HDAC3 with an IC50 of 80 nM and shows >200-fold selectivity for HDAC3 over other HDACs.
Targets |
HDAC3 ( IC50 = 80 nM )
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
Assays for acetylation are derived from the homogenous fluorescence release method. Following pre-incubation periods ranging from 0 to 3 hours, purified recombinant enzymes are incubated in the standard HDAC buffer with serially diluted inhibitors at the concentrations shown in the figures. After pre-incubation, acetyl-Lys(Ac)-AMC substrate (at 10 μM, corresponding to the Km for both HDAC1 and HDAC3) is added. An hour is given for the reaction to continue. An Tecan M200 96-well plate reader is used to measure the fluorescence emission after an hour of adding the trypsin peptidase developer at a final concentration of 5 mg/ml.
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Cell Assay |
At 26105 cells/mL, cells are counted and divided into T25 (Corning) flasks. After that, cells are treated once at hour 0 with either DMSO or HDIs. At 0, 24, 48, and 72 hours following treatment, 100 ml aliquots are taken in triplicate from each flask, distributed into a flat bottom 96-well plate, and 10 ml of alamar blue is added to each well. Using the Biotek Synergy MX Microplate Reader, fluorescence is measured after a 4-hour incubation period.
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Animal Protocol |
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References |
Molecular Formula |
C21H19FN4O
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Molecular Weight |
362.4
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Exact Mass |
362.15
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Elemental Analysis |
C, 69.60; H, 5.28; F, 5.24; N, 15.46; O, 4.41
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CAS # |
1357389-11-7
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Related CAS # |
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Appearance |
White solid powder
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SMILES |
C1=CC=C(C=C1)/C=C/CN2C=C(C=N2)/C=C/C(=O)NC3=C(C=C(C=C3)F)N
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InChi Key |
BLVQHYHDYFTPDV-VCABWLAWSA-N
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InChi Code |
InChI=1S/C21H19FN4O/c22-18-9-10-20(19(23)13-18)25-21(27)11-8-17-14-24-26(15-17)12-4-7-16-5-2-1-3-6-16/h1-11,13-15H,12,23H2,(H,25,27)/b7-4+,11-8+
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Chemical Name |
(E)-N-(2-amino-4-fluorophenyl)-3-[1-[(E)-3-phenylprop-2-enyl]pyrazol-4-yl]prop-2-enamide
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Synonyms |
RGFP966; RGFP-966; RGFP 966
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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 |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.90 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 (6.90 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. View More
Solubility in Formulation 3: 1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL Solubility in Formulation 4: 7.69 mg/mL (21.22 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7594 mL | 13.7969 mL | 27.5938 mL | |
5 mM | 0.5519 mL | 2.7594 mL | 5.5188 mL | |
10 mM | 0.2759 mL | 1.3797 mL | 2.7594 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.