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SKI II

鞘氨醇激酶(SK)抑制剂,SKI II是一种合成的鞘氨醇激酶 (SK) 抑制剂, 抑制SK1和SK2, IC50值分别为78 μM和45 μM。

目录号: PC10763 纯度: ≥98%

CAS No. :312636-16-1

商品编号	规格	价格	会员价
PC10763-25mg	25mg	¥1009.40	请登录
PC10763-100mg	100mg	¥3224.20	请登录
PC10763-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥588.00	请登录

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中文名称

SKI II

中文别名

4-[[4-(4-氯苯基)-2-噻唑基]氨基]苯酚;鞘氨醇激酶抑制剂;4-[[4-(4-氯苯基)-2-噻唑]氨基]苯酚;唑尼沙胺氯

英文名称

SKI II

英文别名

Phenol,4-[[4-(4-chlorophenyl)-2-thiazolyl]amino]-;SKI II;SKI II (SphK-I2);SKI-II;Sphingosine Kinase Inhibitor 2;4-[[4-(4-Chlorophenyl)-2-thiazolyl]amino]phenol

Cas No.

312636-16-1

分子式

C₁₅H₁₁N₂Oscl

分子量

302.78

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

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.

性状

Solid

IC50 & Target[1][2]

IC50 value: 78/45 μM (SK1/2).

体外研究(In Vitro)

SKI II inhibits cell proliferation by suppressing the Wnt/β-catenin signaling pathway. SKI II promotes the degradation of β-catenin by enhancing Wnt5A.
SKI II (1.25 μM, 48 h) in combination with DDP has a clear synergistic effect in human gastric carcinoma SGC7901/DDP cell line.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay

Cell Line:	The human gastric carcinoma SGC7901/DDP cell line.
Concentration:	0 μM, 1.25 μM (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(In Vivo)

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.
SKI II (50.0 mg/kg, IP; 100 mg/kg, PO) treatment reduces tumor growth in mice bearing solid tumor model.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	8 week-old female LDL-R mice.
Dosage:	50.0 mg/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 the maximum (~40%) observed 12 h after injection. At sacrifice (72 h after last injection) S1P levels were 266 ± 18 ng/mL and 328 ± 30 ng/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:	50.0 mg/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:	100 mg/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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Liu H, et al. SphK1 inhibitor SKI II inhibits the proliferation of human hepatoma HepG2 cells via the Wnt5A/β-catenin signaling pathway. Life Sci. 2016 Apr 15;151:23-9. [Information]

[2]. Potì F, et al. SKI-II--a sphingosine kinase 1 inhibitor--exacerbates atherosclerosis in low-density lipoprotein receptor-deficient (LDL-R-/-) mice on high cholesterol diet. Atherosclerosis. 2015 May;240(1):212-5. [Information]

[3]. Liu Y, et al. SKI-II reverses the chemoresistance of SGC7901/DDP gastric cancer cells. Oncol Lett. 2014 Jul;8(1):367-373. [Information]

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

溶解度数据

体外研究:

DMSO : ≥ 100 mg/mL (330.27 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.3027 mL	16.5136 mL	33.0273 mL
5 mM	0.6605 mL	3.3027 mL	6.6055 mL
10 mM	0.3303 mL	1.6514 mL	3.3027 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.75 mg/mL (9.08 mM); Clear solution

此方案可获得 ≥ 2.75 mg/mL (9.08 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.75 mg/mL (9.08 mM); Clear solution

此方案可获得 ≥ 2.75 mg/mL (9.08 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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