Catalog No.S2818 Synonyms: PD-123654, GOE-5549, Acetyldinaline
Molecular Weight(MW): 269.3
Tacedinaline (CI994) is a selective class I HDAC inhibitor with IC50 of 0.9, 0.9, 1.2, and >20 μM for human HDAC 1, 2, 3, and 8, respectively. Phase 3.
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A, 5×106 HeLa, A549, 293T, and H1299 cells were seeded in 10-cm cell culture dishes on day 0 and treated with dimethyl sulfoxide, 10 μM CI994, or 1 μM RGFP966 for 12 h. Cell lysates were collected for Western blotting analysis of Apaf-1 and -actin.
J Biol Chem, 2016, 291(14):7386-95. Tacedinaline (CI994) purchased from Selleck.
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|Description||Tacedinaline (CI994) is a selective class I HDAC inhibitor with IC50 of 0.9, 0.9, 1.2, and >20 μM for human HDAC 1, 2, 3, and 8, respectively. Phase 3.|
CI-994 (< 160 mM) shows cytostatic effect with concomitant increase at G0/G1 phase, a reduction at S phase level and increased apoptosis in A-549 and LX-1 cells.  CI-994 inhibits growth of LNCaP cell with IC50 of 7.4 μM.  CI-994 exerts activity against several tumor cell lines with greater cytotoxicity against the solid tumors relative to both the leukemia and normal fibroblast cell lines.  CI-994 inhibits growth of rat leukemia BCLO cells with IC50 of 2.5 μM. 
|In vivo||CI-994 exerts demonstrated antitumor activity against several tumor models, including the chemo-resistant mouse pancreatic ductal carcinoma as well as the human prostate tumor model LNCaP. |
-  Moradei OM, et al. J Med Chem. 2007, 50(23), 5543-5546.
-  Loprevite M, et al. A Oncol Res, 2005, 15(1), 39-48.
-  Gediya LK, et al. Bioorg Med Chem, 2008, 16(6), 3352-3360.
|In vitro||DMSO||54 mg/mL (200.51 mM)|
|Water||slightly soluble or insoluble|
|Ethanol||slightly soluble or insoluble|
|In vivo||Add solvents individually and in order:
5% DMSO+40% PEG 300+ddH2O
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||PD-123654, GOE-5549, Acetyldinaline|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00005093||Completed||Lung Cancer||Pfizer||December 1999||Phase 3|
|NCT00004861||Completed||Pancreatic Cancer||Pfizer||October 1999||Phase 2|
|NCT00005624||Completed||Multiple Myeloma||H. Lee Moffitt Cancer Center and Research Institute|National Cancer Institute (NCI)|Parke-Davis||August 1997||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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