CD437

CD437 is the prototypical adamantyl arotinoid of the retinoid-related molecule family that acts as a selective agonist of retinoic acid receptor (RAR)γ (Kds = 6.5 μM, 2.5 μM, and 77 nM for RARα, β, and γ, respectively).^1,2 CD437 is cytotoxic to the acute myeloid leukemia cell line NB4 (EC₅₀ = 0.17 μM), inducing DNA damage by producing DNA double strand breaks.³ CD437 also induces cell cycle arrest and apoptosis in various other cancer cells including melanoma, breast, non-small lung, and prostate cancer cells through RAR-dependent and -independent signaling pathways.^4,5

WARNING This product is not for human or veterinary use.

1. Pérez-Rodríguez, S., Ortiz, M.A., Pereira, R., et al. Highly twisted adamantyl arotinoids: Synthesis, antiproliferative effects and RXR transactivation profiles. Eur. J. Med. Chem. 44(6), 2434-2446 (2009).

2. Bernard, B.A., Bernardon, J.-M., Delescluse, C., et al. Identification of synthetic retinoids with selectivity for human nuclear retinoic acid receptor γ. Biochem. Biophys. Res. Commun. 186(2), 977-983 (1992).

3. Valli, C., Paroni, G., Di Francesco, A.M., et al. Atypical retinoids ST1926 and CD437 are S-phase-specific agents causing DNA double-strand breaks: Significance for the cytotoxic and antiproliferative activity. Mol. Cancer Ther. 7(9), 2941-2954 (2008).

4. Fontana, J.A., and Rishi, A.K. Classical and novel retinoids: Their targets in cancer therapy. Leukemia 16(4), 463-472 (2002).

5. Jin, F., Liu, X., Zhou, Z., et al. Activation of nuclear factor-κB contributes to induction of death receptors and apoptosis by the synthetic retinoid CD437 in DU145 human prostate cancer cells. Cancer Res. 65(14), 6354-6363 (2005).