Tacedinaline (CI994)

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

For research use only.

Tacedinaline (CI994, PD-123654, GOE-5549, Acetyldinaline) 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.

Tacedinaline (CI994) Chemical Structure

CAS No. 112522-64-2

Selleck's Tacedinaline (CI994) has been cited by 35 publications

Purity & Quality Control

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Biological Activity

Description Tacedinaline (CI994, PD-123654, GOE-5549, Acetyldinaline) 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]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
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 NEL5TYZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NISyNWE2KGSjeYO= MVjHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDViZHH5d{BjgSCPVGSgZZN{[XluIFfJOVA:OC5zNzFOwG0> MUSxPFU1OzlyMh?=
human PC3 cells NFnQdVJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVn4W4ZlPSCmYYnz M2jwV2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJHBEOyClZXzsd{Bi\nSncjC1JIRigXNiYomgUXRVKGG|c3H5MEBIUTVyPUCuNlkh|ryP NWfsNohmOTh3NEO5NFI>
human HCT116 cells NVWwdoxmS3m2b4TvfIlkyqCjc4PhfS=> M1;VOmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCkeTDNWHQh[XO|YYmsJGlEPTB;NDFOwG0> M1S3VVE4QTRzNkK1
293T cells MV7GeY5kfGmxbjDhd5NigQ>? M3TCV2lvcGmkaYTpc44hd2ZiSFTBR{BqdiB{OUPUJINmdGy|LDDJR|UxRTZizszN NVjVU5RLOTd7NEG2NlU>
human LNCap NWjqPHV6WHKxbHnm[ZJifGmxbjDhd5NigQ>? M3TUUmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF7DZZAh[nliTWTUJIF{e2G778{MJGlEPTB;Nz60JO69VQ>? NGnM[XIyQDF4NkS2OS=>
human NCI-H661 cells MWfQdo9tcW[ncnH0bY9vKGG|c3H5 MU[0PEBp NHzaSm1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JPjZzIHPlcIx{KGGodHXyJFQ5KGi{czygTWM2OD1{MDFOwG0> MYexPFY6OjN7Nx?=
human NCI-H661 cells NIK0b3VHfW6ldHnvckBie3OjeR?= NXXid2NsPiCq M3LKPGlvcGmkaYTpc44hd2ZiSFTBR{BqdiCqdX3hckBPS0lvSE[2NUBk\WyuczDhd5Nme3OnZDDhd{BpcXO2b37lJGg1KGGlZYT5cIF1cW:wIHHmeIVzKDZiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= MkD2NVg3QTJ|OUe=
Assay
Methods Test Index PMID
Growth inhibition assay Cell viability 30108928
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 (from reference)

Cell Research:

[3]

  • 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.

Animal Research:

[4]

  • Animal Models: human prostate tumor model LNCaP
  • Dosages: 535 mg/kg
  • Administration: Administered via oral gavage

Solubility (25°C)

In vitro

DMSO 54 mg/mL
(200.51 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 269.3
Formula

C15H15N3O2

CAS No. 112522-64-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(=O)NC1=CC=C(C=C1)C(=O)NC2=CC=CC=C2N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

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.

Handling Instructions

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