SKI-II - CAS:312636-16-1 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	SKI-II
英文名称:	SKI-II
别名:	SPHK Sphingosine kinase inhibitor II;4-[[4-(4-Chlorophenyl)-2-thiazolyl]amino]phenol
CAS No:	312636-16-1	分子式:	C₁₅H₁₁ClN₂Os	分子量:	302.78
CAS No:	312636-16-1
分子式:	C₁₅H₁₁ClN₂Os
分子量:	302.78

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S10405 SKI-II ≥98%(HPLC) (psaitong)

相关产品

包装规格：

5mg 10mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO(≥100mg/mL)

产品描述：

基本信息

产品编号：	S10405
产品名称：	SKI-II
CAS:	312636-16-1	储存条件	粉末	-20℃	四年

分子式：	C15H11ClN2Os		溶于液体	-80℃	6个月
分子量：	302.78			-20℃	1个月
化学名：	4-[[4-(4-Chlorophenyl)-2-thiazolyl]amino]phenol
Solubility (25°C)：
体外:	DMSO	61mg/mL (201.46mM)
	Ethanol	61mg/mL (201.46mM)
	Water	Insoluble
体内(现配现用):
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	3.3027mL	16.5136mL	33.0273mL
5mM	0.6605mL	3.3027mL	6.6055mL
10mM	0.3303mL	1.6514mL	3.3027mL
50mM	0.0661mL	0.3303mL	0.6605mL

生物活性

产品描述	一种合成的口服有效的鞘氨醇激酶(SK)抑制剂,抑制SK1和SK2。
靶点	Sphingosine Kinase
靶点	0.5μM
体外研究	SKI II inhibits cell proliferation by suppressing the Wnt/β-catenin signaling pathway.SKI II promotes the degradation of βcatenin by enhancing Wnt5A.SKI II (1.25μM,48h) in combination with DDP has a clear synergistic effect in human gastric carcinoma SGC7901/DDP cell line. Cell Cytotoxicity Assay
	Cell Line:	The human gastric carcinoma SGC7901/DDP cell line.
	Concentration:	0μM,1.25μM (combined with DDP).
	Incubation Time:	48 hours.
	Result:	SKI II in combination with DDP had a greater effect on the SGC-7901/DDP cells compared with DDP or SKI II alone.
体内研究	Chronic SKI II (50.0mg/kg,3-weekly i.p.for 16 weeks) administration leads to permanent reduction of S1P concentrations in plasma in mice.SKI II (50.0mg/kg,IP;100mg/kg,PO) treatment reduces tumor growth in mice bearing solid tumor model.
	Animal Model:	8 week-old female LDL-R-/-mice.
	Dosage:	50.0mg/kg.
	Administration:	IP injection daily,3 days a week for 16 weeks.
	Result:	A single administration of produced a significant reduction of plasma S1P with themaximum (~40%) observed 12h after injection.At sacrifice (72h after last injection) S1P levels were 266±18ng/mL and 328±30ng/mL in the SKI-II-treated and control groups,respectively.

	Animal Model:	BALB/c mouse solid tumor model that uses JC mammary adenocarcinoma cells.
	Dosage:	50.0mg/kg.
	Administration:	IP injection daily,3 days a week for 16 weeks.
	Result:	Had strong inhibition of tumor growth from the start of treatment of 65%,with no toxicity or weight loss.

	Animal Model:	BALB/c JC tumor model.
	Dosage:	100mg/kg.
	Administration:	PO every other day.
	Result:	Caused significant antitumor activity in well-established tumors as early as day 5,with maximal response seen at the end of the study. Showed 79% inhibition of tumor growth from the start of treatment.

推荐实验方法(仅供参考)

激酶实验：

SK实验

进行适用于筛选重组人SK抑制剂的中等通量检测。5μg纯化的GST-SK融合蛋白与12nM鞘氨醇[含100倍稀释的[3-3H]鞘氨醇(20 Ci/mmol)],1mM ATP,1mM MgCl2,和200μL实验缓冲液[20mM Tris HCl(pH 7.4),20%甘油,1mM β-巯基乙醇,1mM EDTA,20mM ZnCl2,1mM原钒酸钠,15mM NaF,及0.5mM 4-deoxypyridoxine]结合。实验在25°C下震荡运行30分钟，包含1％DMSO或5g/mL实验化合物，相当于浓度为10-25μM。加入50μL浓(NH4)(OH)终止该反应，然后使用氯仿：甲醇（2:1）提取实验混合物。水相转移到闪烁瓶中，使用Beckman LS 3801闪烁计数器对放射性进行量化，用于测量[3H]]S1P形成。定量检测的批间和批内的变异系数分别为10%和20%。

细胞实验:
细胞系	T-24,MCF-7,MCF-7/VP,NCI/ADR细胞系
浓度	~50μM
处理时间	48小时
方法	T24,MCF-7,MCF-7/VP,和NCI/ADR细胞接种在96孔组织培养板上,达到15％汇合。24小时后，使用各种浓度的抑制剂处理细胞。48小时后，使用Sulforhodamine B法测定细胞存活率