CB1151

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CB1151  纯度: ≥95.0%

CB1151 是 1,25 二羟基维生素D3 (VD) 的 20 表位类似物 ( 20-epi analogue of VD)，具有有效的抗肿瘤作用。CB1151 抑制 MCF-7 细胞生长， IC50 值为 0.82 nM。

CB1151

CB1151 Chemical Structure

CAS No. : 182369-28-4

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生物活性

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].

IC50 & Target

IC50: 0.82 nM[1]
体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

446.66

Formula

C28H46O4
CAS 号

182369-28-4
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]. 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.

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