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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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 M{HMNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYe1JIRigXN? Mke1S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB3IHThfZMh[nliTWTUJIF{e2G7LDDHTVUxRTBwMUeg{txO MXGxPFU1OzlyMh?=
human PC3 cells NGH1NVFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEDDOHU2KGSjeYO= MWTHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiNTDkZZl{KGK7IF3UWEBie3OjeTygS2k2OD1yLkK5JO69VQ>? MUCxPFU1OzlyMh?=
human HCT116 cells MWDDfZRwfG:6aXRCpIF{e2G7 MXvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[nliTWTUJIF{e2G7LDDJR|UxRTRizszN Mn3FNVc6PDF4MkW=
293T cells NEK0eFZHfW6ldHnvckBie3OjeR?= NVfYZVRUUW6qaXLpeIlwdiCxZjDISGFEKGmwIEK5N3Qh[2WubIOsJGlEPTB;NjFOwG0> M1nq[VE4QTRzNkK1
human LNCap NFnPUpVRem:uaX\ldoF1cW:wIHHzd4F6 M1qxOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF7DZZAh[nliTWTUJIF{e2G778{MJGlEPTB;Nz60JO69VQ>? M4PtXlE5OTZ4NE[1
human NCI-H661 cells MX3Qdo9tcW[ncnH0bY9vKGG|c3H5 MWG0PEBp NFSzU3BCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JPjZzIHPlcIx{KGGodHXyJFQ5KGi{czygTWM2OD1{MDFOwG0> M1zISlE5Pjl{M{m3
human NCI-H661 cells NUi5dZhQTnWwY4Tpc44h[XO|YYm= M3nxTVYhcA>? MUTJcohq[mm2aX;uJI9nKEiGQVOgbY4hcHWvYX6gUmNKNUh4NkGgZ4VtdHNiYYPz[ZN{\WRiYYOgbIl{fG:wZTDIOEBi[2W2eXzheIlwdiCjZoTldkA3KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MnXSNVg3QTJ|OUe=

... 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 5% DMSO+40% PEG 300+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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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HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID