Vorinostat (SAHA, MK0683) |
| Catalog No.: GC17390 |
Vorinostat (SAHA, MK0683) (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC6 and HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively.
Sample solution is provided at 25 µL, 10mM.
;)
;)
;)
;)
;)
;)
;)
;)
;)
;)
;)
;)
;)
;)
;)
;)
Quality Control & SDS
- View current batch:
-
Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment: [1] | |
|
Cell lines |
Human cutaneous T-cell lymphomas (CTCL) cell lines |
|
Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
|
Reaction Conditions |
IC50: 0.146 μM HH 2.062 μM HuT78 2.697 μM MJ 1.375 μM MylA 1.510 μM SeAx 72h |
|
Applications |
Vorinostat dose-dependently reduced cell proliferation with IC50 values of 0.146 μM, 2.062 μM, 2.697 μM, 1.375 μM and 1.510 μM in HH, HuT78, MJ, MylA and SeAx cells, respectively. |
| Animal experiment : [2] | |
|
Animal models |
C57BL/6 mice bearing Eμ-myc lymphomas |
|
Dosage form |
C57BL/6 mice bearing Eμ-myc lymphomas were injected with vorinostat (200 mg/kg i.p.) and lymphoma cells were harvested after the indicated time points. The percentage of tumor cells in the lymph node of C57BL/6mice bearing Eμ-myc lymphomas treated with vorinostat was determined by FACS analysis. |
|
Applications |
Vorinostat induced a marked accumulation of Eμ-myc lymphomas displaying DNA fragmentation in vivo. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1] Wozniak M B, Villuendas R, Bischoff J R, et al. Vorinostat interferes with the signaling transduction pathway of T cell receptor and synergizes with PI3K inhibitors in cutaneous T-cell lymphoma. haematologica, 2010: haematol. 2009.013870. [2] Lindemann R K, Newbold A, Whitecross K F, et al. Analysis of the apoptotic and therapeutic activities of histone deacetylase inhibitors by using a mouse model of B cell lymphoma. Proceedings of the National Academy of Sciences, 2007, 104(19): 8071-8076. |
|
Vorinostat (suberoylanilide hydroxamic acid, SAHA) is a histone deacetylase inhibitor (HDACi), that plays key roles in epigenetic or non-epigenetic regulation, inducing growth arrest, differentiation and apoptosis of tumor cells.[1] Vorinostat is a small molecular with the formular of C14H20N2O3 and molecular weight of 264.3. The major mechanism of HDACi-induced apoptosis is the activation of the intrinsic apoptotic pathway. HDACi can activate the intrinsic apoptotic pathway by releasing of cytochrome c from mitochondria and regulating of Bcl-2 family expression.[2]
Reference
[1] Hui-ming Z, Qian-hai D, Wei-ping C, Ru-bin L. Vorinostat, a HDAC inhibitor, showed anti-osteoarthritic activities through inhibition of iNOS and MMP expression, p38 and ERK phosphorylation and blocking NF-kB nuclear translocation. International Immunopharmacology. 2013, 17. 329-335.
[2] Norihisa U, Sayaka K, Hisanori M, Katsuhiko Y, Airo T. Requirement of p38 MAPK for a cell-death pathway triggered by vorinostat in MDA-MB-231 human breast cancer cells. Cancer Letters. 2012, 315. 112-121.
| Cas No. | 149647-78-9 | SDF | |
| Synonyms | SAHA, suberoylanilide hydroxamic acid, Suberanilohydroxamic acid, SAHA cpd | ||
| Chemical Name | N'-hydroxy-N-phenyloctanediamide | ||
| Canonical SMILES | C1=CC=C(C=C1)NC(=O)CCCCCCC(=O)NO | ||
| Formula | C14H20N2O3 | M.Wt | 264.3 |
| Solubility | ≥ 4.4 mg/mL in DMSO, <2.45 mg/mL in EtOH, <2.61 mg/mL in Water | Storage | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
||
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Abstract
The MTD, DLT and PK properties of vorinostat, an HDAC inhibitor, were determined in a study utilizing vorinostat plus temozolomide to treat children with refractory or recurrent CNS malignancies.
Abstract
The efficacy and tolerability of vorinostat plus bortezomib were assessed in multiple myeloma patients.
Abstract
Vorinostat, a class I/II HDAC inhibitor, alters the expression of target genes and induces cell cycle arrest and apoptosis.
Abstract
Although it’s been used to treat advanced CTCL patients, vorinostat, a HDACi with anti-cancer activity, is currently being evaluated to treat other solid tumors and hematological malignancies.
Abstract
The effect of vorinostat, which is a HDACi capable of inducing cell-cycle arrest, apoptosis and differentiation, on biomarker modulation in women with breast cancer was evaluated.
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *