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SKI II

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Chemical Structure| 312636-16-1 同义名 : Sphingosine Kinase Inhibitor 2;SphK-I2;SKI II. Sphingosine kinase inhibitor II
CAS号 : 312636-16-1
货号 : A122860
分子式 : C15H11ClN2OS
纯度 : 99%+
分子量 : 302.779
MDL号 : MFCD00733553
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(346.79 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Sphingosine kinase is a conserved lipid kinase that catalyzes formation sphingosine-1-phosphate, which is a key promotor in cancer. SKI-II is an oral active and synthetic inhibitor of sphingosine kinase (SK) activity, with IC50 values of 78 μM and 45 μM for SK1 and for SK2, respectively. SKI II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation. SKI II (1.25 μM, 48 h) in combination with DDP has a clear synergistic effect in human gastric carcinoma SGC7901/DDP cell line[3]. Chronic SKI II (50.0 mg/kg, 3-weekly i.p. for 16 weeks) administration leads to permanent reduction of S1P concentrations in plasma in mice[4]. SKI II (50.0 mg/kg, IP; 100 mg/kg, PO) treatment reduces tumor growth in mice bearing solid tumor model[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.30mL

0.66mL

0.33mL

16.51mL

3.30mL

1.65mL

33.03mL

6.61mL

3.30mL
参考文献

[1]French KJ, Upson JJ, et al. Antitumor activity of sphingosine kinase inhibitors. J Pharmacol Exp Ther. 2006 Aug;318(2):596-603.

[2]French KJ, Schrecengost RS, et al. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 2003 Sep 15;63(18):5962-9.

[3]Potì F, Ceglarek U, Burkhardt R, Simoni M, Nofer JR. SKI-II--a sphingosine kinase 1 inhibitor--exacerbates atherosclerosis in low-density lipoprotein receptor-deficient (LDL-R-/-) mice on high cholesterol diet. Atherosclerosis. 2015;240(1):212-215.

[4]Liu Y, Zhu Z, Cai H, Liu Q, Zhou H, Zhu Z. SKI-II reverses the chemoresistance of SGC7901/DDP gastric cancer cells. Oncol Lett. 2014;8(1):367-373.

[5]French KJ, Upson JJ, Keller SN, Zhuang Y, Yun JK, Smith CD. Antitumor activity of sphingosine kinase inhibitors. J Pharmacol Exp Ther. 2006;318(2):596-603.