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CD437

Cat. No. M7719
CD437 Structure
Synonym:

AHPN; Ro-472077

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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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
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 398.49
Formula C27H26O3
CAS Number 125316-60-1
Purity >98%
Solubility DMSO: 100 mg/mL (Need ultrasonic and warming)
Storage at -20°C
References

Molecular determinants of AHPN (CD437)-induced growth arrest and apoptosis in human lung cancer cell lines.
Li Y, et al. Mol Cell Biol. 1998 Aug;18(8):4719-31. PMID: 9671482.

Treatment of melanoma cells with the synthetic retinoid CD437 induces apoptosis via activation of AP-1 in vitro, and causes growth inhibition in xenografts in vivo.
Schadendorf D, et al. J Cell Biol. 1996 Dec;135(6 Pt 2):1889-98. PMID: 8991099.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CD437, AHPN; Ro-472077 supplier, RAR/RXR, inhibitors

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