CB1151

CB1151 is a 20-epi analogue of 1,25 dihydroxyvitamin D3 (VD) with potent anti-tumor effects. CB1151 inhibits MCF-7 cell growth with an IC50 value of 0.82 nM[1].

Research Areas >> Cancer

Signaling Pathways >> Vitamin D Related >> VD/VDR

IC50: 0.82 nM[1]

CB1151 (0-100 nM; 5 days) inhibits MCF-7 cells growth, this cell proliferation is accessed by [3H]-thymidine incorporation, exhibits an IC50 value of 0.82 nM[1]. CB1151 (0-100 nM; 40 hours) exhibits activation of the IP9-type VD response element with a EC50 of 1.2 nM, the activation of IP9-type VD response elements shows a good correlation with inhibition of proliferation than the activation of DR3-type elements (EC50=3.2nM) in MCF-7 cells transfected with the CAT reporter[1]. CB1151 shows a functional dissociation constant (Kdf) value of 3.6 nM. The ligand concentration that provides 50% of protease-resistant VDR fragment is defined by Kdf, this is different from that of the traditional dissociation constant (Kd)[2]. Cell Proliferation Assay[1] Cell Line: MCF-7 cell Concentration: 0 nM; 0.1nM; 0.5nM; 0.8nM; 1nM; 5nM; 10 nM Incubation Time: 5 days Result: Inhibits MCF-7 cells growth.

[1]. Mørk Hansen C, et al. The potent anti-proliferative effect of 20-epi analogues of 1,25 dihydroxyvitamin D3 in human breast-cancer MCF-7 cells is related to promoter selectivity.Int J Cancer. 1996 Sep 4;67(5):739-42.

[2]. Nayeri S, et al. High-affinity nuclear receptor binding of 20-epi analogues of 1,25-dihydroxyvitamin D3 correlates well with gene activation.J Cell Biochem. 1996 Sep 1;62(3):325-33.