Vorinostat(SAHA)

Modify Date: 2024-01-02 18:08:37

Vorinostat(SAHA) Structure
Vorinostat(SAHA) structure
Common Name Vorinostat(SAHA)
CAS Number 149647-78-9 Molecular Weight 264.320
Density 1.2±0.1 g/cm3 Boiling Point N/A
Molecular Formula C14H20N2O3 Melting Point 161-162°C
MSDS Chinese USA Flash Point N/A
Symbol GHS08
GHS08
Signal Word Danger

 Use of Vorinostat(SAHA)


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.

 Names

Name vorinostat
Synonym More Synonyms

 Vorinostat(SAHA) Biological Activity

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.
Related Catalog
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.
References

[1]. Hrzenjak A et al. Histone deacetylase inhibitor vorinostat suppresses the growth of uterine sarcomas in vitro and in vivo. Mol Cancer. 2010 Mar 4;9:49.

[2]. Lautz TB, et al. The effect of vorinostat on the development of resistance to Doxorubicin in neuroblastoma.PLoS One. 2012;7(7):e40816.

[3]. Richon VM, et al. A class of hybrid polar inducers of transformed cell differentiation inhibits histone deacetylases. Proc Natl Acad Sci U S A. 1998 Mar 17;95(6):3003-7.

[4]. Xu WS, et al. Histone deacetylase inhibitors: molecular mechanisms of action. Oncogene. 2007 Aug 13;26(37):5541-52.

[5]. Pérez-Cañamás A, et al. Sphingomyelin-induced inhibition of the plasma membrane calcium ATPase causes neurodegeneration in type A Niemann-Pick disease. Mol Psychiatry. 2017 May;22(5):711-723.

[6]. Wang J, et al. Snail determines the therapeutic response to mTOR kinase inhibitors by transcriptional repression of 4E-BP1. Nat Commun. 2017 Dec 20;8(1):2207.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Melting Point 161-162°C
Molecular Formula C14H20N2O3
Molecular Weight 264.320
Exact Mass 264.147400
PSA 78.43000
LogP 0.86
Index of Refraction 1.567
Storage condition -20°C Freezer

 Synthetic Route

 Customs

HS Code 2924299090
Summary 2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

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 Synonyms

SAHA
Suberoylanilidehydroxamic Acid
N-Hydroxy-N'-phenyloctanediamide
M344
Vorinostat/SAHA
Vorinostat
suberoylanilide hydroxamic acid
suberanilohydroxamic acid
Zolinza
Octanediamide, N-hydroxy-N-phenyl-
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