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Vorinostat(SAHA)
| Product Name | Vorinostat(SAHA) |
| Price: | Inquiry |
| Catalog No.: | CN00553 |
| CAS No.: | 149647-78-9 |
| Molecular Formula: | C14H20N2O3 |
| Molecular Weight: | 264.3 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | ONC(=O)CCCCCCC(=O)Nc1ccccc1 |
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| Description | Vorinostat is a potent and orally available inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV ), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. |
| Target | HDAC1:10 nM (ID50) HDAC3:20 nM (ID50) HDAC2 HDAC7 HDAC11 Mitophagy Autophagy |
| In Vitro | Vorinostat efficiently suppresses MES-SA cell growth at a low dosage (3 μM) already after 24 hours treatment. HDACs class I (HDAC2 and 3) as well as class II (HDAC7) are preferentially affected by this treatment. Vorinostat significantly increases p21WAF1 expression and apoptosis in MES-SA cells[1]. Vorinostat inhibits SK-N-SH and SK-N-Be(2)C with the IC25 values of 1 µM and 0.5 µM, respectively[2]. |
| In Vivo | Vorinostat (50 mg/kg/day) reduces tumor growth by more than 50% in nude mice injected with 5×106 MES-SA cells[1]. |
| Cell Assay | Cell lysates are prepared by using RIPA buffer (25 mM Tris-HCl pH 7.6, 150 mM NaCl, 1% NP-40, 1% sodium deoxycholate, 0.1% SDS), and the protein concentration is determined by Bio-Rad DC Protein Assay. Protein lysates are separated by SDS-PAGE and transferred to nitrocellulose membrane. Following antibodies and dilutions are used: rabbit anti HDAC1 (1 μg/mL); rabbit anti HDAC2 (1 μg/mL); rabbit anti HDAC3 (9 μg/mL); rabbit anti HDAC7 (3 μg/mL); mouse anti p21WAF1 (0.5 μg/mL). As secondary antibodies, the rabbit anti-mouse and swine anti-rabbit HRP-coupled antibodies at a final concentration of 1 μg/mL. An overnight incubation at 4°C is used for all primary antibodies, followed by washing and 2-hours incubation at RT with secondary antibodies. Specific protein bands are visualized by enhanced chemiluminescence assay. To demonstrate equal loading of protein samples all western blots are probed for β-tubulin. |
| Animal Admin | Twelve weeks old male mice (n=14) are anesthetized with Isofluran and 5×106 MES-SA cells are injected subcutaneously into the right flank of the animal. Mice from a control group receives placebo containing 300 μL of empty HOP-β-CD (2-hydroxypropyl-β-cyclodextrin) vesicles. Another group of mice receives vorinostat dissolved in HOP-β-CD at a concentration of 50 mg/kg/day. Both, empty vesicles and vorinostat are administered intraperitoneally, starting on the day 4 after the injection of MES-SA tumor cells. Mice body weight and tumor size (w2 × l × 0.52; measured by caliper) are estimated twice a week. All mice are treated for 21 days and afterwards sacrificed by cervical dislocation. Each tumor is isolated as a whole and different tumor parameters are determined. Finally, tumor slices are cryo preserved and formalin fixed (4%) for further analyses. |
| Density | 1.2±0.1 g/cm3 |
| Exact Mass | 264.147400 |
| PSA | 78.43000 |
| LogP | 0.86 |
| Storage condition | -20°C Freezer |