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Cat. No. M2236
CI-994 Structure

Tacedinaline, PD 123654

Size Price Availability Quantity
10mM/1mL In DMSO USD 55 In stock
10mg USD 50 In stock
50mg USD 120 In stock
100mg USD 180 In stock
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Quality Control
Biological Activity

CI-994 (N-acetyldinaline) is a novel oral agent which inhibits HDAC1, with a wide spectrum of antitumor activity in preclinical models, in vitro and in vivo. CI-994 inhibits growth of LNCaP cell with IC50 of 7.4 μM. CI-994 inhibits growth of rat leukemia BCLO cells with IC50 of 2.5 μM. The effect of CI-994, as demonstrated by recovery experiments, was cytostatic and seemed to be superimposable in both cell lines. Cytofluorimetric analysis to assess cell cycle perturbation and apoptosis was performed after 24 h of treatment, indicating a cell block with concomitant increase at G0/G1 phase, a reduction at S phase level at 20, 40, 80, and 160 microM, and apoptosis at the higher concentration (160 microM). CI-994 is currently in a phase III clinical trial in patients with lung cancer.

Customer Product Validations & Biological Datas
Source AIDS Res Hum Retroviruses (2016). Figure 3. CI-994
Method Immunoblots
Cell Lines CD4+ T cells
Concentrations 0.57 μM
Incubation Time 24 h
Results Both vorinostat and panobinostat, but not tacedinaline, increased CDK9 T-loop phosphorylation in CCL19-treated cells compared to control cells. Vorinostat and panobinostat, but not tacedinaline, also increased histone H3 acetylation in CCl19-treated cells.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 269.3
Formula C15H15N3O2
CAS Number 112522-64-2
Purity >99%
Solubility DMSO 50 mg/mL
Storage at -20°C
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Abmole Inhibitor Catalog 2017

Keywords: CI-994, Tacedinaline, PD 123654 supplier, HDAC, inhibitors

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