Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Tacedinaline (GOE5549, PD123654, CI994; Acetyldinaline) is a potent, orally bioavailable and selective inhibitor of histone deacetylase 1/3 (HDAC1/3) with potential anticancer activity. It has IC50s of 0.9, 0.9, and 1.2 μM for HDAC1/2/3 inhibition, respectively.
Targets |
HD1 ( IC50 = 0.9 μM ); HD2 ( IC50 = 0.9 μM ); HD3 ( IC50 = 1.2 μM )
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
Tacedinaline, also known as N-acetyldinaline, has IC50 values of 0.9, 0.9, and 1.2 μM for recombinant HDAC 1, 2, and 3, respectively, making it an inhibitor of histone deacetylase (HDAC).
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Cell Assay |
The whole culture medium of RPMI 1640 medium, which includes 10% fetal bovine serum, 1% penicillin, and 1% streptomycin, is used to maintain LNCaP cell lines. 24-well plates are seeded with 2×104 cells, which are then incubated for one day at 37 °C in an incubator with 5% CO2. On days two and four, cultures are treated with CI-994 both alone and in combination. On days two and four, media are replaced and cells are cleaned. As a gauge of cell proliferation, mitochondrial metabolism is assessed by introducing 100 μL/well MTT (5 mg/mL in medium) and incubating it for two hours at 37 °C on Day 6. Dissolved crystals are placed in 500 μL of DMSO. At 560 nm, the absorbance is measured with a microplate reader. The percentage of cell proliferation is calculated from the absorbance data. Three duplicates of each assay are run.
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Animal Protocol |
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References |
Molecular Formula |
C15H15N3O2
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Molecular Weight |
269.3
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Exact Mass |
269.12
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Elemental Analysis |
C, 66.90; H, 5.61; N, 15.60; O, 11.88
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CAS # |
112522-64-2
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Appearance |
Off-white solid powder
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SMILES |
CC(=O)NC1=CC=C(C=C1)C(=O)NC2=CC=CC=C2N
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InChi Key |
VAZAPHZUAVEOMC-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C15H15N3O2/c1-10(19)17-12-8-6-11(7-9-12)15(20)18-14-5-3-2-4-13(14)16/h2-9H,16H2,1H3,(H,17,19)(H,18,20)
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Chemical Name |
4-acetamido-N-(2-aminophenyl)benzamide
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Synonyms |
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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) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.7133 mL | 18.5667 mL | 37.1333 mL | |
5 mM | 0.7427 mL | 3.7133 mL | 7.4267 mL | |
10 mM | 0.3713 mL | 1.8567 mL | 3.7133 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00005624 | Completed | Drug: CI-994 | Multiple Myeloma | H. Lee Moffitt Cancer Center and Research Institute |
August 1997 | Phase 2 |
NCT00005093 | Completed | Drug: gemcitabine hydrochloride Drug: tacedinaline |
Lung Cancer | Pfizer | December 1999 | Phase 3 |
NCT00004861 | Completed | Drug: gemcitabine hydrochloride Drug: tacedinaline |
Pancreatic Cancer | Pfizer | October 1999 | Phase 2 |