Vorinostat Inhibitor CAS No. 149647-78-9

Cat. No.	Name	Size	Price	Add Cart
KI0176	Vorinostat	250 mg	$148
KI0176	Vorinostat	1 g	$446

Chemical Characteristic

Product Name	Vorinostat
Synonyms	Suberoylanilide hydroxamic acid, SAHA, Zolinza
CAS No.	149647-78-9
Molecular Weight	264.32
Formula	C₁₄H₂₀N₂O₃
Chemical Name	N1-?hydroxy-?N8-?phenyl-octanediamide
Smiles	C(=O)(CCCCCCC(=O)NO)Nc1ccccc1
Chemical Structure
Documents	HPLC MS COA

Biological activities

Vorinostat is a HDAC1 (histone deacetylases) inhibitor. The IC50 of vorinostat is 85 nM against HDAC1.^[1] HDAC inhibitor vorinostat enhances the antitumor effect of gefitinib in squamous cell carcinoma of head and neck by modulating ErbB receptor expression and reverting EMT (epithelial-to-mesenchymal transition).^[2] Vorinostat at a dose of 1 µM inhibits the growth of A549, 128-88T, Calu1 and 201T cells by 17%, 28%, 39% and 41%, respectively. Vorinostat synergistically increases the growth inhibitory effects of carboplatin/paclitaxel in 128-88T cells. In A549, combination of vorinostat with paclitaxel results in a synergistic increase in tubulin acetylation. The IC50 of vorinostat is 1.94 and 1.69 µM against A549 cells and 128-88T cells, respectively, while that of vorinostat is 1.29 and 1.21 µM, against 201T cells and Calu 1 cells, respectively. Vorinostat increases carboplatin-induced DNA damage in A549 and 128-88T cells. Vorinostat potentiates paclitaxel-induced apoptosis and reversibly increases -tubulin acetylation in NSCLC (non-small cell lung cancer) cells.^[3] Vorinostat alters the cell cycle distribution of 231-BR cells, with an increased percentage of cells in the G0-G1 phases (43% versus 62-70% of cells) and a corresponding decrease in S phase (37% versus 10-15%), indicative of a G1-S blockade. Vorinostat also inhibits the clonogenic growth and migration of 231-BR cells.^[4] Irradiation of s.c. MDA-MB-231-BR tumors in mice treated with vorinostat results in an increase in radiation-induced tumor growth delay. Most importantly, animals with intracranial tumor implants live the longest after combination treatment of irradiation and vorinostat.^[5] Subeffective vorinostat doses markedly increases carfilzomib (CFZ)-mediated tumor growth suppression and apoptosis in a murine xenograft OCI-LY10 model.^[6]

Protocols

Vorinostat is dissolved in DMSO as 5 mM stock solutions and kept at room temperature. ^[2]

References

[1] Arts J, et al. JNJ-26481585, a novel "second-generation" oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity. Clin Cancer Res. 2009, 15(22): 6841-6851. [2] Bruzzese F, et al. HDAC inhibitor vorinostat enhances the antitumor effect of gefitinib in squamous cell carcinoma of head and neck by modulating ErbB receptor expression and reverting EMT. J Cell Physiol. 2011, 226(9): 2378-2390. [3] Owonikoko TK, et al. Vorinostat increases carboplatin and paclitaxel activity in non-small-cell lung cancer cells. Int J Cancer. 2010, 126(3): 743-755. [4] Palmieri D, et al. Vorinostat inhibits brain metastatic colonization in a model of triple-negative breast cancer and induces DNA double-strand breaks. Clin Cancer Res. 2009, 15(19): 6148-6157. [5] Baschnagel A, et al. Vorinostat enhances the radiosensitivity of a breast cancer brain metastatic cell line grown in vitro and as intracranial xenografts. Mol Cancer Ther. 2009, 8(6): 1589-1595. [6] Dasmahapatra G, et al. The pan-HDAC inhibitor vorinostat potentiates the activity of the proteasome inhibitor carfilzomib in human DLBCL cells in vitro and in vivo. Blood. 2010, 115(22): 4478-4487.

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