产品说明书

OSI-027

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Chemical Structure| 936890-98-1 同义名 : ASP7486;CERC 006;AEVI-006;ASP4786
CAS号 : 936890-98-1
货号 : A419082
分子式 : C21H22N6O3
纯度 : 99%+
分子量 : 406.438
MDL号 : MFCD20275101
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(258.34 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

1% DMSO+30% polyethylene glycol+1% Tween 80+water 30 mg/mL suspension

生物活性
靶点

  • mTORC1

    mTORC1, IC50:22 nM

  • mTORC2

    mTORC2, IC50:65 nM

  • mTOR

    mTOR, IC50:4 nM
描述 The mammalian target of rapamycin (mTOR) is a serine/threonine kinase that integrates with multiple pathways involving cell growth, survival and cancer physiology. OSI-027 is an ATP-competitive inhibitor of mTOR kinase with an IC50 value of 4 nM. OSI-027 targeted both mTORC1 and mTORC2 , the two complexes of mTOR, with IC50 values of 22 and 65 nM, respectively. In mechanistic cell assay, OSI-027 inhibited mTOR signaling of phospho-4E-BP1 with an IC50 value of 1 μM. Treatment with OSI-027 (0.001 - 10 μΜ) dose-dependently suppressed Akt phosphorylation and the downstream substrate of Akt, PRAS40, in ovcar-3 ovarian carcinoma cells[3]. In acute myeloid leukemia (AML) cells, OSI-027 blocked mTORC1 and mTORC2 activities at the concentration of 10 μΜ. The incubation with 10 μΜ OSI-027 also suppressed the mRNA translation of cyclin D1 and other proliferation-related genes in AML cells[4]. In GEO colorectal xenograft mice, administration of OSI-027 (65 mg/kg) for 12 days inhibited both mTORC1 and mTORC2 effectors, and slowed the tumor growth as compared to the control group[3].
作用机制 OSI-027 is a ATP-competitive inhibitor of mTOR kinase.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human Caki1 cells Cytotoxicity assay 72 h Cytotoxicity against human Caki1 cells after 72 hrs by MTT assay, IC50=1.9 μM 24445311
human COLO205 cells Cytotoxicity assay 72 h Cytotoxicity against human COLO205 cells after 72 hrs by MTT assay, IC50=5.8 μM 24445311
human COLO205 cells Cytotoxicity assay 72 h Cytotoxicity against human COLO205 cells after 72 hrs by MTT assay 24836070
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.30mL

2.46mL

1.23mL

24.60mL

4.92mL

2.46mL
参考文献

[1]Falcon BL, Barr S, Gokhale PC, Chou J, Fogarty J, Depeille P, Miglarese M, Epstein DM, McDonald DM. Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors. Cancer Res. 2011 Mar 1;71(5):1573-83. doi: 10.1158/0008-5472.CAN-10-3126. PMID: 21363918; PMCID: PMC3077087.

[2]Altman JK, Sassano A, Kaur S, Glaser H, Kroczynska B, Redig AJ, Russo S, Barr S, Platanias LC. Dual mTORC2/mTORC1 targeting results in potent suppressive effects on acute myeloid leukemia (AML) progenitors. Clin Cancer Res. 2011 Jul 1;17(13):4378-88. doi: 10.1158/1078-0432.CCR-10-2285. Epub 2011 Mar 17. PMID: 21415215; PMCID: PMC3131493.