SKI II - CAS:312636-16-1

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SKI II

目录号 : KM6710 CAS No. : 312636-16-1 纯度 : 98%

Data Sheet 产品使用指南

SKI II 是一种合成的、口服有效的鞘氨醇激酶 (SK) 抑制剂, 抑制 SK1 和 SK2, IC₅₀值分别为 78 μM 和 45 μM。SKI II 通过诱导溶酶体和/或蛋白酶体降解导致SK1的不可逆抑制。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg		In-stock
500mg	询价	In-stock
1g	询价	In-stock

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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.

体外研究

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.

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

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.

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.

分子式

C₁₅H₁₁N₂Oscl

分子量

302.78

CAS号

312636-16-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (330.27 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

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

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

请依序添加每种溶剂： 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。
2.

请依序添加每种溶剂： 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。