product name CI994 (Tacedinaline)
Description: CI994 is a selective HDAC1 and HDAC3. When tested with HeLa cervical carcinoma cells, CI994 treatment showed a selectivity inhibitory ability for HDAC1 and 3 with the IC50 was 43.5±1.2 μM. In peripheral blood lymphocytes isolated from untreated male Wistar rats, administration of CI994 for 24 hours induced cells apoptosis in a dose-dependent manner (1 μM~10μM ). In NSCLC cell lines (A549 and LX-1), CI994 administration induced cell apoptosis via inhibiting HDAC activity and arresting cell cycle at G0/G1 phase and showed a promising therapy strategy when combined with chemotherapy.
References: J Med Chem. 2007;50(23):5543-6; Bioorg Med Chem. 2008;16(6):3352-60; Invest New Drugs. 1996;14(4):349-56.
269.3
Formula
C15H15N3O2
CAS No.
112522-64-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 54 mg/mL (200.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
Synonyms
PD-123654, GOE-5549, Acetyldinaline, Tacedinaline
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19425684
| In Vitro |
In vitro activity: 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. CI-994 inhibits growth of LNCaP cell with IC50 of 7.4 μM. 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. CI-994 inhibits growth of rat leukemia BCLO cells with IC50 of 2.5 μM. Kinase Assay: Cell Assay: 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. |
|---|---|
| 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. |
| Animal model | Human prostate tumor model LNCaP |
| Formulation & Dosage | Dissolved in 5% ethanol, 1% P.O.E. and 94% dH20; Oral gavage |
| References | J Med Chem. 2007 Nov 15;50(23):5543-6; Oncol Res. 2005;15(1):39-48; Bioorg Med Chem. 2008 Mar 15;16(6):3352-60; Invest New Drugs. 1996;14(4):349-56. |
