CI994 (Tacedinaline)

Catalog No.S2818 1 Product Citations

CI-994 (Tacedinaline) is an anti-cancer drug which inhibits HDAC1 with IC50 of 0.57 μM and causes G1 cell cycle arrest. Phase 3.

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CI994 (Tacedinaline) Chemical Structure

CI994 (Tacedinaline) Chemical Structure
Molecular Weight: 269.3

Validation & Quality Control

Quality Control & MSDS

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Product Information

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  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description CI-994 (Tacedinaline) is an anti-cancer drug which inhibits HDAC1 with IC50 of 0.57 μM and causes G1 cell cycle arrest. Phase 3.
Targets HDAC1 [1]
IC50 0.57 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]
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]
Features

Protocol(Only for Reference)

Cell Assay: [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 Study: [4]

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
Solubility 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Methot JL, et al. Bioorg Med Chem Lett, 2008, 18(3), 973-978.

[2] Loprevite M, et al. A Oncol Res, 2005, 15(1), 39-48.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-12-13)

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|Natio  ...more H. Lee Moffitt Cancer Center and Research Institute|National Cancer Institute (NCI)|Parke-Davis August 1997 Phase 2

Chemical Information

Download CI994 (Tacedinaline) SDF
Molecular Weight (MW) 269.3
Formula

C15H15N3O2

CAS No. 112522-64-2
Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms PD-123654, GOE-5549, Acetyldinaline
Solubility (25°C) * In vitro DMSO 54 mg/mL (200.51 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 30 mg/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 Name Benzamide, 4-(acetylamino)-N-(2-aminophenyl)-

Research Area

Product Citations (1)

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