SKI V|cas:24418-86-8|西域试剂

SKI V,98.09%

产品编号：Bellancom-12895| CAS NO：24418-86-8| 分子式：C₁₅H₁₀O₄| 分子量：254.24

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货号	价格	库存与货期
Bellancom-12895	￥2800.00	杭州北京（现货）
Bellancom-12895	￥4500.00	杭州北京（现货）
Bellancom-12895	￥12500.00	杭州北京（现货）
Bellancom-12895	￥0.00	杭州北京（现货）

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SKI V

产品介绍

SKI V 是一种非竞争性的，有效的非脂质鞘氨醇激酶 (SPHK; SK) 抑制剂，对 GST-hSK 的 IC₅₀ 为 2 μM。 SKI V 有效抑制 PI3K，对 hPI3k 的 IC₅₀ 为 6 μM。SKI V 减少有丝分裂的第二信使鞘氨醇-1-磷酸 (S1P) 的形成。SKI V 诱导细胞凋亡 (apoptosis) 并具有抗肿瘤活性。

生物活性

SKI V is a noncompetitive and potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with an IC₅₀ of 2 μM for GST-hSK. SKI V potently inhibits PI3K with an IC₅₀ of 6 μM for hPI3k. SKI V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P). SKI V induces apoptosis and has antitumor activity.

体外研究

SKI V has weak activity toward ERK2 (IC₅₀ of 80 μM for hERK2) and does not inhibit PKC-α.
SKI V (10 μM; for 24 hours) inhibits cancer cell proliferation and induces apoptosis.
SKI V (0.2, 1, 5 μM; pretreated for 1 hour) decreases phospho-Akt and phospho-MEK levels. Near-confluent cultures of JC cells are serum-starved for 16 hours, followed by pretreatment SKI V for 1 hour.
SKI V has IC₅₀s for inhibition of sphingosine kinase (SK) and tumor cell proliferation of ∼2 μM.
SKI V (20 μg/ml) inhibits not only purified but endogenous SK in in MDA-MB-231 cells.
SKI V (0.2, 1, 5 μM) inhibits intracellular S1P formation in JC cells in a dose-dependent fashion.

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

Cell Proliferation Assay

Cell Line:	T24 tumor cells
Concentration:	10 μM
Incubation Time:	For 24 hours
Result:	Inhibited cancer cell proliferation.

Apoptosis Analysis

Cell Line:	T24 tumor cells
Concentration:	10 μM
Incubation Time:	For 24 hours
Result:	Induced apoptosis.

Western Blot Analysis

Cell Line:	JC cells
Concentration:	0.2, 1, 5 μM
Incubation Time:	Pretreated for 1 hour
Result:	Decreased phospho-Akt and phospho-MEK levels.

体内研究
(In Vivo)

SKI V (75 mg/kg; i.p.; days 1, 5, 9, 15) significantly lowers tumor growth (>50% decreased at day 18) than control animals.

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

Animal Model:	6-8 weeks old BALB/c female mice with JC mammary adenocarcinoma cells
Dosage:	75 mg/kg
Administration:	IP; days 1, 5, 9, 15
Result:	Tumor growth was significantly lower (>50% decreased at day 18) than tumor growth in control animals.

体内研究

SKI V (75 mg/kg; i.p.; days 1, 5, 9, 15) significantly lowers tumor growth (>50% decreased at day 18) than control animals.

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

Animal Model:	6-8 weeks old BALB/c female mice with JC mammary adenocarcinoma cells
Dosage:	75 mg/kg
Administration:	IP; days 1, 5, 9, 15
Result:	Tumor growth was significantly lower (>50% decreased at day 18) than tumor growth in control animals.

体内研究

SKI V (75 mg/kg; i.p.; days 1, 5, 9, 15) significantly lowers tumor growth (>50% decreased at day 18) than control animals.

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

Animal Model:	6-8 weeks old BALB/c female mice with JC mammary adenocarcinoma cells
Dosage:	75 mg/kg
Administration:	IP; days 1, 5, 9, 15
Result:	Tumor growth was significantly lower (>50% decreased at day 18) than tumor growth in control animals.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (196.66 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.9333 mL	19.6665 mL	39.3329 mL
5 mM	0.7867 mL	3.9333 mL	7.8666 mL
10 mM	0.3933 mL	1.9666 mL	3.9333 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: ≥ 2.5 mg/mL (9.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.83 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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 ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (9.83 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (9.83 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 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