Tacedinaline (CI994)

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Technical Data

Molecular Weight 269.3 Storage powder
Formula

C15H15N3O2

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CAS No. 112522-64-2 Synonyms PD-123654, GOE-5549, Acetyldinaline
Solubility (25°C) * In vitro DMSO 54 mg/mL (200.51 mM)
Water Insoluble
Ethanol Insoluble
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 Name Benzamide, 4-(acetylamino)-N-(2-aminophenyl)-

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]
(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]
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
 

References

Customer Product Validation

Data from [Data independently produced by , , J Biol Chem, 2016, 291(14):7386-95]

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.

Data from [Data independently produced by , , Cell Oncol (Dordr), 2017, 40(3):263-279]

Apoptosis marker analysis. Daoy and D283 Med cells were exposed to various HDACi 24 h before total RNA samples were prepared for qRT-PCR. Daoy cells were exposed to DMSO, 25 nM TSA, 1 μM SAHA, 1.5 μM MS-275, 0.7 μM mocetinostat, 7 μM tacedinaline, 1.5 nM romidepsin and 2 μM parthenolide, respectively. D283 Med cells were exposed to DMSO, 40 nM TSA, 1.5 μM SAHA, 2 μM MS-275, 0.3 μM mocetinostat, 8 μM tacedinaline, 1 nM romidepsin and 4 μM parthenolide, respectively. Expression of the apoptosis markers BAX and BCL2, as well as the apoptotic BAX/BCL2 ratios, are shown. * p < 0.05; **p < 0.01.

Tacedinaline (CI994) has been referenced in 4 publications.

PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.

Specific storage and handling information for each product is indicated on the product datasheet. Most Selleck products are stable under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage temperature. Short-term storage of many products are stable in the short-term at temperatures that differ from that required for long-term storage.
We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, follow the storage recommendations on the product data sheet.

Chemical Structure

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