2. Cell Cycle/DNA Damage
    Epigenetics
    Apoptosis
  3. HDAC
    Apoptosis
  4. Tacedinaline

Tacedinaline  (Synonyms: N-acetyldinaline; CI-994; Goe-5549)

Cat. No.: HY-50934 Purity: 99.55%
COA Handling Instructions

Tacedinaline (N-acetyldinaline) is an inhibitor of the histone deacetylase (HDAC) with IC50s of 0.9, 0.9, 1.2 μM for recombinant HDAC 1, 2 and 3 respectively.

For research use only. We do not sell to patients.

Tacedinaline Chemical Structure

Tacedinaline Chemical Structure

CAS No. : 112522-64-2

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Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
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ready for reconstitution
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Estimated Time of Arrival: December 31
Solid
10 mg USD 55 In-stock
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50 mg USD 83 In-stock
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100 mg USD 121 In-stock
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200 mg USD 211 In-stock
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500 mg USD 449 In-stock
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Based on 4 publication(s) in Google Scholar

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Description

Tacedinaline (N-acetyldinaline) is an inhibitor of the histone deacetylase (HDAC) with IC50s of 0.9, 0.9, 1.2 μM for recombinant HDAC 1, 2 and 3 respectively.

IC50 & Target[1]

HD1

0.9 μM (IC50)

HD2

0.9 μM (IC50)

HD3

1.2 μM (IC50)

In Vitro

Tacedinaline (N-acetyldinaline) is a novel oral compound with a wide spectrum of antitumor activity in preclinical models. The mechanism of action may involve inhibition of histone deacetylation and cell cycle arrest. Tacedinaline (N-acetyldinaline) is combined with antineoplastic agents commonly used in non-small cell lung cancer cell line management, a marked synergism of action (R=1.8, R=1.5) is observed between Tacedinaline (N-acetyldinaline) (40 μM) and gemcitabine (0.01 μM) at 48 and 72 h of treatment[2]. Tacedinaline (N-acetyldinaline) inhibits mitogen-stimulated blood lymphocyte proliferation with an IC50 value of 3 μM[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

Tacedinaline (CI-994) has activity against 8/8 solid tumors tested: pancreatic ductal adenocarcinoma #02 (4.7); pancreatic adenocarcinoma #03 (3.0; 1/6 cures); colon adenocarcinoma #38 (1.6); colon adenocarcinoma #51/A (1.1); mammary adenocarcinoma #25 (1.7); mammary adenocarcinoma #17/ADR (0.5); Dunning osteogenic sarcoma (4.0); and the human prostate carcinoma LNCaP (1.2). CI-994 is the acetylated metabolite of dinaline and has the same spectrum of activity in vivo as dinaline. It also behaves similarly in schedule comparison/toxicity trials[3]. Tacedinaline (CI-994) can effect lymphoid tissue in rats within 1 day of a single oral dose, that effects are generally reversible within 7 days[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

269.30

Appearance

Solid

Formula

C15H15N3O2
CAS No.
SMILES

O=C(NC1=C(N)C=CC=C1)C2=CC=C(NC(C)=O)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (185.67 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7133 mL 18.5667 mL 37.1333 mL
5 mM 0.7427 mL 3.7133 mL 7.4267 mL
10 mM 0.3713 mL 1.8567 mL 3.7133 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.28 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.55%

COA (246 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[4]

Rats: To characterize the effects of Tacedinaline (CI-994) on lymphoid tissue, male rats are administered single oral doses at 0 (vehicle control), 10, 23, and 45 mg/kg and killed up to 7 days after dosing for evaluation of white blood cell differentials, bone marrow differentials, lymphoid tissue weights, and selected histopathology of lymphoid tissue[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Tacedinaline112522-64-2N-acetyldinaline CI-994 Goe-5549CI994CI 994CI-994Goe5549Goe 5549Goe-5549HDACApoptosisHistone deacetylasesInhibitorinhibitorinhibit

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