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.
Apoptosis marker analysis. Daoy and D283 Med cells were exposed to various HDACi 24 h before total RNA samples were prepared for qRT-PCR. Daoy cells were exposed to DMSO, 25 nM TSA, 1 μM SAHA, 1.5 μM MS-275, 0.7 μM mocetinostat, 7 μM tacedinaline, 1.5 nM romidepsin and 2 μM parthenolide, respectively. D283 Med cells were exposed to DMSO, 40 nM TSA, 1.5 μM SAHA, 2 μM MS-275, 0.3 μM mocetinostat, 8 μM tacedinaline, 1 nM romidepsin and 4 μM parthenolide, respectively. Expression of the apoptosis markers BAX and BCL2, as well as the apoptotic BAX/BCL2 ratios, are shown. * p < 0.05; **p < 0.01.
Cell Oncol (Dordr), 2017, 40(3):263-279. 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)|
|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|
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