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CD437 is a retinoic acid receptor (RAR)γ-selective agonist, γ-selective retinoid; potent inducer of apoptosis. It displays RARγ-dependent and -independent effects on differentiation and apoptosis. CD437 reduces the numbers of H460, SK-MES-1, A549, and H292 cells with 50% inhibitory values of approximately 0.5, 0.4, 3, and 0.85 μM, respectively. Treatment for 72 h with CD437 causes a strong dose-dependent growth inhibition in all melanoma cell lines. At a concentration of 5 μM CD437, only about 5 to 25% of the cells remain viable after 3 d. The concentrations of CD437 required for 50% growth inhibition (IC50) range from 10 μM for MeWo to 0.1 μM for SK-Mel-23 showing the highest sensitivity.
In vivo, tumors in CD437-treated mice stop growing, an effect that becomes already statistically significant (P<0.01) at day 13, 3 d after first administration of CD437, and is maintained for more than 3 wk after discontinuation of treatment. Further histologic analysis demonstrates marked c-fos mRNA levels at the tumor-stroma edge in CD437-treated tumors.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Male Swiss-nu/nu mice weighing 20 to 25 g |
| Formulation | |
| Dosages | 10 mg/kg/body weight and 30 mg/kg/body weight |
| Administration | injected intratumorally or fed |
| Molecular Weight | 398.49 |
| Formula | C27H26O3 |
| CAS Number | 125316-60-1 |
| Solubility (25°C) | DMSO: 100 mg/mL (Need ultrasonic and warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related RAR/RXR Products |
|---|
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YCT529 is a potent, selective and orally active RAR-α inhibitor. |
| LG101506
LG101506 is a selective and orally active RXR modulator with a Ki of 2.7 nM for RXRα. |
| ER 50891
ER-50891 is a potent antagonist of retinoic acid receptor α(RARα). |
| LG100754
LG100754 (UVI 2112) is a RXR dimers modulater. |
| AGN 196996
AGN 196996 is a potent and selective RARα antagonist with Ki value of 2 nM; little binding affinity for RARβ(Ki=1087 nM) and RARγ(Ki=8523 nM). |
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