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OSI-027

OSI-027 (ASP4786) 是一种选择性、可口服和 ATP 竞争性的mTOR 激酶活性抑制剂，IC50为 4 nM。它抑制mTORC1和mTORC2，IC50分别为 22 nM 和 65 nM。

CAS号

936890-98-1

分子式

C21H22N6O3

主要靶点

PI3K|Autophagy|DNA-PK|mTOR

仅限科研使用

Cat No : CM05228

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Synonyms

OSI027|ASP4786

验证数据展示

  • CAS No.: 936890-98-1

    OSI-027
    CAS#: 936890-98-1

产品信息

OSI-027 (ASP4786) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. Phase 1.

CAS号 936890-98-1
分子式 C21H22N6O3
主要靶点 PI3K|Autophagy|DNA-PK|mTOR
主要通路 PI3K/Akt/mTOR信号通路|DNA损伤和修复|自噬
分子量 406.44
纯度 98.00%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 OSI027|ASP4786

靶点活性

mTORC1:22 nM|mTORC2:65 nM

体内活性

In GEO colorectal xenograft, OSI-027 (65 mg/kg) inhibits both mTORC1 and mTORC2 effectors, including 4E-BP1, Akt, and S6 phosphorylation. Furthermore, mTORC1 and mTORC2 inhibition together by OSI-027 potently inhibits tumor growth more than mTORC1 inhibition by rapamycin. [1]

体外活性

OSI-027 shows the selective and ATP competitive inhibition activities against mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively. In addition, OSI-027 inhibits mTOR signaling of phospho-4E-BP1 with an IC50 of 1 μM in cell-based assays. [1] OSI-027 exhibits anti-proliferative activities against several acute leukemia cell lines of myeloid/megakaryocytic origin in a dose-dependent manner, including U937, KG-1, KBM-3B, ML-1, HL-60, and MEG-01 cells. [2] A recent study shows that inhibition of mTORC1/2 by OSI-027 effectively suppresses phosphorylation of Akt (S473) and cell proliferation in breast cancer cells. [3]

溶解度

Ethanol:<1 mg/mL,H2O:<1 mg/mL,DMSO:15 mg/mL (36.9 mM)

细胞实验

Inhibition of proliferation is measured using the Cell Titer Glo Assay , as noted in figure legends. To generate dose–response curves, cell lines are seeded at a density of 5,000 cells per well in a 96-well plate. After 24 hours of plating, cells are dosed with varying concentrations of either OSI-027 or rapamycin. The signal for Cell Titer Glo Assay is determined 72 hours after dosing and normalized to that of vehicle-treated controls. Inhibition of proliferation, relative to vehicle-treated controls, is expressed as a fraction of 1 and graphed using PRISM software. (Only for Reference)

参考文献

1.Falcon BL, et al. Cancer Res, 2011, 71(5), 1573-1583.
2.Altman JK, et al. Clin Cancer Res, 2011, 17(13), 4378-4388.
3.Li H, et al. Breast Cancer Res Treat, 2012, 134(3), 1057-1066.
4.Bhagwat SV, et al. Mol Cancer Ther. 2011, 10(8), 1394-1406.
5.Zhi X, et al. OSI-027 modulates acute graft-versus-host disease after liver transplantation in a rat model. Liver Transpl. 2017 Sep;23(9):1186-1198.

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