OSU-03012

目录号 M1848 所有产品仅供科研使用，严禁用于人或动物的治疗等任何其他用途，不为任何个人提供产品和服务

OSU-03012 (AR-12)是一种有效的重组PDK-1抑制剂，IC50为5 μM，比OSU-02067作用效果高2倍。

别名：OSU03012

规格	价格	库存状态
Free Sample (0.5-1 mg)	¥ 0	中国库存现货
5mg	¥ 513	中国库存现货
10mg	¥ 765	中国库存现货
25mg	¥ 1683	中国库存现货
50mg	¥ 2871	中国库存现货
100mg	¥ 4995	中国库存现货

其他规格数量报价？

质量标准及产品资料

纯度： >99%
COA
MSDS
H-NMR
HPLC

产品信息

生物活性

OSU-03012 (AR-12)是一种有效的重组PDK-1抑制剂，IC50为5 μM，比OSU-02067作用效果高2倍。OSU-03012诱导PC-3细胞凋亡，IC50为5 µM，且降低免疫沉淀的p70S6K的活性。Celecoxib完全抑制肿瘤细胞生长,浓度至少需要50 μM，而OSU-03012浓度为3-5 μM时即可完全抑制多种肿瘤细胞生长。与作用于正常的胶质细胞相比，OSU-03012作用于神经胶质瘤细胞更有效促进细胞死亡。

产品使用成果展示

	数据来源	Mol Med Rep (2015). Figure 2.OSU‑03012
	方法	Apoptosis detection
	细胞系/动物模型	LX2 cells
	浓度	1 μM
	处理时间	48 or 72 h
	实验结果	Aapoptosis was not induced in LX2 cells treated with OSU‑03012, compared with those treated with DMSO. These results indicated that OSU‑03012 did not inhibit the growth of LX2 cells via the induction of apoptosis.

实验参考

体外实验*
细胞系	VS and HMS-97 cells
方法	Cell proliferation assay VS and HMS-97 cells were grown in polylysine/laminin-coated 96-well plates (5 × 103 to 1 × 104 per well). After incubation at 37°C for 24 hrs, cells were treated with various concentrations of OSU-03012 or DMSO as a vehicle control at 37°C for another 48 hrs. To assess cell proliferation, the CellTiter 96®AQueous One Solution Cell Proliferation Assay (Promega) was used according to the manufacturer’s instructions. Briefly, 20μl of CellTiter 96® AQueous One Solution Reagent were added to each well and incubated at 37°C for 1 to 4 hrs. The amount of colored formazan produced in the cells was measured at 490nm using a Victor3 1420 Multilabel Counter (Perkin Elmer). The percentage of cell proliferation was plotted against the concentrations of OSU-03012, and the IC50 (defined as the drug concentration at which the population of viable cells was reduced by 50%) was determined using CalcuSyn software (Biosoft). The experiments were replicated six times, and the mean IC50 was calculated.
浓度	0~16µM
处理时间	48h

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

体内实验*
动物模型	Schwannoma xenografts in severe combined immunodeficiency mice (SCID)
配制	methylcellulose (0.5%, w/v) and Tween 80 (0.1%, w/v) in sterile water
剂量	200 mg/kg/day
给药处理	oral gavage

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

化学性质

分子量	460.45
分子式	C26H19F3N4O
CAS号	742112-33-0
溶解性（25°C）	DMSO ≥11 mg/mL
储存条件	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.1718 mL	10.8589 mL	21.7179 mL
5 mM	0.4344 mL	2.1718 mL	4.3436 mL
10 mM	0.2172 mL	1.0859 mL	2.1718 mL

不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
重量 (kg)	0.02	0.15	1.8	0.4	0.08	10
体表面积 (m²)	0.007	0.025	0.15	0.05	0.02	0.5
K_m 系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的K_m系数
	动物 A的K_m系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Booth et al. Cancer Biol Ther. OSU-03012 suppresses GRP78/BiP expression that causes PERK-dependent increases in tumor cell killing.

[2] Jackson et al. Am J Physiol Renal Physiol. Endogenous adenosine contributes to renal sympathetic neurotransmission via postjunctional A1 receptor-mediated coincident signaling.

[3] Oviedo-Boyso et al. Infect Immun. The phosphoinositide-3-kinase-Akt signaling pathway is important for Staphylococcus aureus internalization by endothelial cells.

[4] Yamamoto et al. Biomed Res. OSU-03012, a novel celecoxib derivative, induces cell swelling and shortens action potential duration in mouse ventricular cells.

[5] Hamed et al. Cancer Biol Ther. OSU-03012 enhances Ad.7-induced GBM cell killing via ER stress and autophagy and by decreasing expression of mitochondrial protective proteins.

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