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Purity: ≥98%
In a test without cells, it inhibits HDACs (pooled HDACs with all isoforms) with an IC50 of less than 10 nM. With ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively, it inhibits HDAC1, HDAC2, and HDAC3 (Class I), HDAC7 (Class II), and HDAC11 (Class IV). It has been demonstrated that vorinostat binds to the histone deacetylases' active site and functions as a chelator for the zinc ions that are likewise present there. Because vorinostat inhibits histone deacetylases, acetylated proteins and histones accumulate, which is essential for cell differentiation. The FDA approved SAHA, also known as Vorinostat, in October 2006, making it the first HDAC inhibitor to treat rare cutaneous T-cell lymphoma.
Targets |
HDAC1 ( IC50 = 10 nM ); HDAC3 ( IC50 = 20 nM ); HDAC2; HDAC7; HDAC11; Autophagy; Mitophagy
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
The Jurkat cell lysate is treated with ice for an hour before being centrifuged at 12,000 g for ten minutes at 4 °C to remove any remaining material. 30 μL of 50% protein G-Sepharose slurry is added to supernatants and left for an hour at 4 °C to preclearase them. Using either the homologous or heterologous immunizing peptide, beads are pelleted by centrifugation, and the supernatants are then incubated for 1 hour at 4 °C with 10 μg of IgG fraction from anti-HDAC1 or HDAC3 polyclonal antisera (preincubated for 2 hours at room temperature). Rabbits are used to raise both antisera against the carboxylterminal peptide of HDAC1 and HDAC3, using synthetic peptides coupled to keyhole limpet hemocyanin). Half an hour is spent at 4°C with 30 μL of a 50% protein G-Sepharose slurry added. After centrifuging the immune complexes, 1 mL of lysis buffer is used to wash them three times. A 3H-acetylated peptide that corresponds to amino acids 1 through 24 of histone H4 is used in the HDAC assay, and beads are resuspended in 200 μL of HDAC buffer (20 mM Tris-HCl, pH 8.0/150 mM NaCl/10% glycerol). By using scintillation counting, released [3H]acetic acid is measured. Vorinostat at varying concentrations is preincubated with the immunoprecipitated complexes for 30 minutes at 4 °C in order to conduct inhibitions studies.
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Cell Assay |
RIPA buffer (25 mM Tris-HCl pH 7.6, 150 mM NaCl, 1% NP-40, 1% sodium deoxycholate, 0.1% SDS) is used to prepare cell lysates, and the Bio-Rad DC Protein Assay is used to measure the protein concentration. Protein lysates are moved to nitrocellulose membrane after being separated via SDS-PAGE. The subsequent dilutions and antibodies are utilized: mouse anti-p21WAF1 (0.5 μg/mL), rabbit anti-HDAC1 (1 μg/mL), rabbit anti-HDAC2 (1 μg/mL), rabbit anti-HDAC3 (9 μg/mL), and rabbit anti-HDAC7 (3 μg/mL). The swine anti-rabbit and rabbit anti-mouse HRP-coupled antibodies were used as secondary antibodies, with a final concentration of 1 μg/mL. All primary antibodies are incubated at 4°C for an entire night before being washed and secondary antibodies are incubated at room temperature for two hours. The enhanced chemiluminescence assay allows for the visualization of particular protein bands. In order to exhibit uniform loading of protein samples, β-tubulin is probed on every western blot.
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Animal Protocol |
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References |
[1]. Proc Natl Acad Sci U S A . 1998 Mar 17;95(6):3003-7. [2]. Cancer Res . 2000 Sep 15;60(18):5165-70. [3]. Cancer Res . 2001 Dec 1;61(23):8492-7. [4]. Proc Natl Acad Sci U S A . 2003 Feb 18;100(4):2041-6. [5]. Proc Natl Acad Sci U S A . 2004 Jan 13;101(2):540-5. [6]. Clin Cancer Res . 2004 Jun 1;10(11):3839-52. |
Molecular Formula |
C14H20N2O3
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Molecular Weight |
264.3
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Exact Mass |
264.15
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Elemental Analysis |
C, 63.62; H, 7.63; N, 10.60; O, 18.16
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CAS # |
149647-78-9
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Appearance |
White to off-white solid powder
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SMILES |
C1=CC=C(C=C1)NC(=O)CCCCCCC(=O)NO
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InChi Key |
WAEXFXRVDQXREF-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C14H20N2O3/c17-13(15-12-8-4-3-5-9-12)10-6-1-2-7-11-14(18)16-19/h3-5,8-9,19H,1-2,6-7,10-11H2,(H,15,17)(H,16,18)
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Chemical Name |
N'-hydroxy-N-phenyloctanediamide
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Synonyms |
MK0683; SAHA; M344; CCRIS 8456; CCRIS8456; CCRIS-8456; HSDB 7930; Vorinostat; suberoylanilide hydroxamic acid; MK-0683; MK 0683; MK0683; M344; HSDB 7930; Trade name: Zolinza
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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) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.7836 mL | 18.9179 mL | 37.8358 mL | |
5 mM | 0.7567 mL | 3.7836 mL | 7.5672 mL | |
10 mM | 0.3784 mL | 1.8918 mL | 3.7836 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 |
NCT01236560 | Active Recruiting |
Drug: Vorinostat Drug: Temozolomide |
Brain Stem Glioma Cerebral Astrocytoma |
National Cancer Institute (NCI) |
November 15, 2010 | Phase 2 Phase 3 |
NCT01281176 | Active Recruiting |
Drug: Vorinostat Drug: Carboplatin |
Adult Solid Neoplasm | National Cancer Institute (NCI) |
February 9, 2011 | Phase 1 |
NCT02638090 | Active Recruiting |
Drug: Vorinostat Drug: Pembrolizumab |
Non-small Cell Lung Cancer Lung Cancer |
H. Lee Moffitt Cancer Center and Research Institute |
March 22, 2016 | Phase 1 Phase 2 |
NCT00268385 | Active Recruiting |
Drug: Vorinostat Drug: Temozolomide |
Adult Glioblastoma Adult Gliosarcoma |
National Cancer Institute (NCI) |
December 16, 2005 | Phase 1 |
NCT02737046 | Active Recruiting |
Drug: Vorinostat Drug: Sargramostim |
Neuroblastoma | New Approaches to Neuroblastoma Therapy Consortium |
September 12, 2018 | Phase 1 |