For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I017272 |
| CAS Number | 182369-28-4 |
| Synonyms | (1R,3S,5Z)-5-[(2E)-2-[(1S,3aS,7aS)-1-[(1R)-1-(3-ethyl-3-hydroxypentoxy)ethyl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol |
| Molecular Formula | C28H46O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C28H46O4/c1-6-28(31,7-2)15-16-32-20(4)24-12-13-25-21(9-8-14-27(24,25)5)10-11-22-17-23(29)18-26(30)19(22)3/h10-11,20,23-26,29-31H,3,6-9,12-18H2,1-2,4-5H3/b21-10+,22-11-/t20-,23-,24-,25+,26+,27-/m1/s1 |
| InChIKey | MJTTZPJXKAGWID-BSGGSXJLSA-N |
| SMILES | CCC(CC)(CCOC(C)C1CCC2C1(CCCC2=CC=C3CC(CC(C3=C)O)O)C)O |
| Reference | [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. |
