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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 |
|---|
| Acitretin (Ro 10-1670)
Acitretin (Ro 10-1670) is a second-generation retinoid. |
| Adapalene
Adapalene is a third-generation topical retinoid, it is a potent RAR agonist, with AC50 values of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene is also an MST1 agonist. |
| Tamibarotene
Tamibarotene is a synthetic retinoic acid receptor (RAR) agonist with high specificity for RARα and RARβ over RARγ. |
| TTNPB
TTNPB (Arotinoid Acid) is a potent RAR agonist, and inhibits binding of [3H]tRA with IC50 of 5.1 nM, 4.5 nM, and 9.3 nM for human RARα, β, and γ, respectively. |
| Fenretinide
Fenretinide (4-HPR) is a synthetic retinoid deriverative. Fenretinide is shown to exhibit binding to the retinoic acid receptors (RAR) at concentrations necessary to induce cell death. |
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