OSU-T315

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OSU-T315  纯度: 99.21%

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。

OSU-T315

OSU-T315 Chemical Structure

CAS No. : 2070015-22-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3520 In-stock
5 mg ￥3000 In-stock
10 mg ￥5000 In-stock
50 mg ￥13000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

OSU-T315 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Cytoskeleton Compound Library
  • Anti-Breast Cancer Compound Library

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)[1]. OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner[2]. OSU-T315 causes cell death through apoptosis and autophagy[1].

IC50 & Target

IC50: 0.6μM; Integrin-linked kinase (ILK) inhibitor[1]
体外研究
(In Vitro)

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[1].
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[1].
OSU-T315 (0-4 μM; 24 hours) causes autophagy through ILK inhibition[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis [1]

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 [1]

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[1]

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 [1].
No other obvious toxicity is observed in mice[1].

上海金畔生物科技有限公司 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).

分子量

533.59

Formula

C30H30F3N5O
CAS 号

2070015-22-2
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 : ≥ 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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Su-Lin Lee,et al Identification and Characterization of a Novel Integrin-Linked Kinase Inhibitor.J Med Chem. 2011 Sep 22; 54(18): 6364–6374

    [2]. Liu TM, et al. OSU-T315: a novel targeted therapeutic that antagonizes AKT membrane localization and activation of chronic lymphocytic leukemia cells. Blood. 2015 Jan 8;125(2):284-95.

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