Tacedinaline (CI994)

Catalog No.S2818 Synonyms: PD-123654, GOE-5549, Acetyldinaline

Tacedinaline (CI994) Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 270 In stock
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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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Biological Activity

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.
Targets
HDAC1 [1]
(Cell-free assay)
HDAC2 [1] HDAC3 [1]
0.9 μM 0.9 μM 1.2 μM
In vitro

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. [2] CI-994 inhibits growth of LNCaP cell with IC50 of 7.4 μM. [3] 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. [4] CI-994 inhibits growth of rat leukemia BCLO cells with IC50 of 2.5 μM. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MDA-MB-231 cells MlrrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUjzS|FDPSCmYYnz NX;GRopST3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bi\nSncjC1JIRigXNiYomgUXRVKGG|c3H5MEBIUTVyPUCuNVch|ryP NFG2dlQyQDV2M{mwNi=>
human PC3 cells M4jyVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkLXOUBl[Xm| NWnqTWVrT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hWEN|IHPlcIx{KGGodHXyJFUh\GG7czDifUBOXFRiYYPzZZktKEeLNUC9NE4zQSEQvF2= NXHNcXl1OTh3NEO5NFI>
human HCT116 cells NGO1cnpEgXSxdH;4bYPDqGG|c3H5 NUfQRYZWS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME20JO69VQ>? MkPtNVc6PDF4MkW=
293T cells MYPGeY5kfGmxbjDhd5NigQ>? Mnv6TY5pcWKrdHnvckBw\iCKRFHDJIlvKDJ7M2SgZ4VtdHNuIFnDOVA:PiEQvF2= M1;B[FE4QTRzNkK1
human LNCap MUTQdo9tcW[ncnH0bY9vKGG|c3H5 Mnv2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOTlPhdEBjgSCPVGSgZZN{[XoxvJygTWM2OD15LkSg{txO M3jwXFE5OTZ4NE[1
human NCI-H661 cells MXzQdo9tcW[ncnH0bY9vKGG|c3H5 M3HLclQ5KGh? MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IOlYyKGOnbHzzJIFnfGW{IES4JIhzeyxiSVO1NF0zOCEQvF2= NIn4VpIyQDZ7MkO5Oy=>
human NCI-H661 cells MWrGeY5kfGmxbjDhd5NigQ>? MkHEOkBp NHjoWJBKdmirYnn0bY9vKG:oIFjERWMhcW5iaIXtZY4hVkOLLVi2OlEh[2WubIOgZZN{\XO|ZXSgZZMhcGm|dH;u[UBJPCCjY3X0fYxifGmxbjDh[pRmeiB4IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= M33kfFE5Pjl{M{m3

... Click to View More Cell Line Experimental Data

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. [4]

Protocol

Cell Research:

[3]

+ Expand
  • Cell lines: LNCaP cell lines
  • Concentrations: 2.5 μM
  • Incubation Time: 2-4 days
  • Method:

    LNCaP cell lines are maintained in RPMI 1640 medium containing 10% fetal bovine serum, 1% penicillin and streptomycin, as the complete culture medium. Cells (2×104) are seeded in 24-well plates and incubated in a 5% CO2 incubator at 37 °C for 1 day. Cultures are treated with CI-994, alone and in combination on day 2 and 4. Cells are washed on day 2 and 4 and media are changed. Mitochondrial metabolism is measured as a marker for cell growth by adding 100 μL/well MTT (5 mg/mL in medium) with 2 hours incubation at 37 °C on Day 6. Crystals formed are dissolved in 500 μL of DMSO. The absorbance is determined using a microplate reader at 560 nm. The absorbance data are converted into cell proliferation percentage. Each assay is performed in triplicate.


    (Only for Reference)
Animal Research:

[4]

+ Expand
  • Animal Models: human prostate tumor model LNCaP
  • Formulation: 5% ethanol, 1% P.O.E. and 94% dH20
  • Dosages: 535 mg/kg
  • Administration: Administered via oral gavage
    (Only for Reference)

Solubility (25°C)

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
5mg/mL

* 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.

Chemical Information

Molecular Weight 269.3
Formula

C15H15N3O2

CAS No. 112522-64-2
Storage powder
in solvent
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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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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HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID