OSU-T315|cas:2070015-22-2|西域试剂

OSU-T315,99.21%

产品编号：Bellancom-18676| CAS NO：2070015-22-2| 分子式：C₃₀H₃₀F₃N₅O| 分子量：533.59

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货号	价格	库存与货期
Bellancom-18676	￥3000.00	杭州北京（现货）
Bellancom-18676	￥5000.00	杭州北京（现货）
Bellancom-18676	￥13000.00	杭州北京（现货）

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OSU-T315

产品介绍

OSU-T315 是整联蛋白连接激酶 (ILK) 的抑制剂 (IC₅₀=0.6 μM), 通过去磷酸化 AKT-Ser473 和其他 ILK 靶标 (GSK-3β和肌球蛋白轻链) 抑制 PI3K/AKT 信号传导。 OSU-T315 阻止 AKT 转位到脂筏消除 AKT 的活化，并以 ILK 非依赖性方式触发 Caspase 依赖性细胞凋亡 (Apoptosis)。OSU-T315 通过自噬 (Autophagy) 和凋亡 (Apoptosis) 导致细胞死亡。

生物活性

OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC₅₀ of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and autophagy.

体外研究

OSU-T315 (Compound 22; 0-5 μM; 24 hours) exhibits high in vitro potency against a panel of prostate and breast cancer cell lines with a IC₅₀ range of 1-2.5 μM.
OSU-T315 (0-2.5 μM; 24 hours) can reduce YB-1, HER2, and EGFR expression; shows a modest suppressive effect on phosphorylated S6 levels, exhibits dose-dependent suppressive effects on the levels of phospho-ERK1/2 and phospho-p38, while that of phospho-JNK remains unaltered in PC-3 cell.
OSU-T315 (0-4 μM; 24 hours) causes autophagy through ILK inhibition.

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

Western Blot Analysis

Cell Line:	PC-3 cells; MDA-MB-231 cells
Concentration:	1 μM, 2 μM, 3 μM, 4 μM; 0.5 μM, 1 μM, 1.5 μM, 2 μM, 2.5 μM
Incubation Time:	24 hours
Result:	Exhibited a dose-dependent decreasing effect on the phosphorylation of pS6, ERKs, and p38 in PC-3 cells and MDA-MB-231 cells.

Cell Viability Assay

Cell Line:	Prostate cancer cells: LNCaP, PC-3; breast cancer cells: MDA-MB-231, MDA-MB-468, SKBR3, MCF-7; PrEC and MEC cells
Concentration:	0-5 μM
Incubation Time:	24 hours
Result:	Suppressed cancer cells viability in breast and prostate cancer cells (IC (50), 1-2.5μM).

Apoptosis Analysis

Cell Line:	PC-3 cells
Concentration:	1 μM, 2 μM, 3 μM, 4 μM
Incubation Time:	24 hours
Result:	Induced accumulation of LC3-II and PARP cleavage.

体内研究
(In Vivo)

OSU-T315 (Oral gavage; 25 mg/kg, 50 mg/kg; single daily; 35 days) has a suppressive effect of on PC-3 xenograft tumor growth .
No other obvious toxicity is observed in mice.

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

Animal Model:	Male NCr athymic nude mice with PC-3 tumor xenografts
Dosage:	25 mg/kg; 50 mg/kg
Administration:	Oral gavage; single daily; 35 days
Result:	Resulted in suppression of tumor growth relative to the vehicle control after 35 days of treatment (48% and 62% suppression for 25 and 50 mg/kg, respectively).

体内研究

OSU-T315 (Oral gavage; 25 mg/kg, 50 mg/kg; single daily; 35 days) has a suppressive effect of on PC-3 xenograft tumor growth .
No other obvious toxicity is observed in mice.

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

Animal Model:	Male NCr athymic nude mice with PC-3 tumor xenografts
Dosage:	25 mg/kg; 50 mg/kg
Administration:	Oral gavage; single daily; 35 days
Result:	Resulted in suppression of tumor growth relative to the vehicle control after 35 days of treatment (48% and 62% suppression for 25 and 50 mg/kg, respectively).

体内研究

OSU-T315 (Oral gavage; 25 mg/kg, 50 mg/kg; single daily; 35 days) has a suppressive effect of on PC-3 xenograft tumor growth .
No other obvious toxicity is observed in mice.

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

Animal Model:	Male NCr athymic nude mice with PC-3 tumor xenografts
Dosage:	25 mg/kg; 50 mg/kg
Administration:	Oral gavage; single daily; 35 days
Result:	Resulted in suppression of tumor growth relative to the vehicle control after 35 days of treatment (48% and 62% suppression for 25 and 50 mg/kg, respectively).

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 260 mg/mL (487.27 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	1.8741 mL	9.3705 mL	18.7410 mL
5 mM	0.3748 mL	1.8741 mL	3.7482 mL
10 mM	0.1874 mL	0.9370 mL	1.8741 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: ≥ 2.17 mg/mL (4.07 mM); Clear solution

此方案可获得 ≥ 2.17 mg/mL (4.07 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 21.7 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% corn oil
Solubility: ≥ 2.17 mg/mL (4.07 mM); Clear solution

此方案可获得 ≥ 2.17 mg/mL (4.07 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。