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 IC 50 value of 0.82 nM.
性状
Solid
IC50 & Target[1][2]
IC50: 0.82 nM
体外研究(In Vitro)
CB1151 (0-100 nM; 5 days) inhibits MCF-7 cells growth, this cell proliferation is accessed by [H]-thymidine incorporation, exhibits an IC50 value of 0.82 nM.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. 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).
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
参考文献
[1]. M?rk 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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (223.88 mM; Need ultrasonic)配制储备液