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Sapanisertib

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Chemical Structure| 1224844-38-5 同义名 : INK-128;TAK-228;MLN0128
CAS号 : 1224844-38-5
货号 : A121801
分子式 : C15H15N7O
纯度 : 99%+
分子量 : 309.326
MDL号 : MFCD22124893
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: 55 mg/mL(177.81 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：

IP 2% DMSO+2% Tween80+30% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 71 mg/mL suspension

生物活性
靶点

  • mTOR

    mTOR, Ki:1.4 nM
描述 Sapanisertib (INK-128) demonstrates enzymatic inhibitory activity against mTOR with over 100-fold selectivity compared to PI3K kinases[1]. Sapanisertib (INK-128) selectively reduces the protein levels of YB1, MTA1, vimentin, and CD44 without affecting their mRNA levels in PC3 cells. It also diminishes the invasive capabilities of PC3 prostate cancer cells. Additionally, Sapanisertib (INK-128) impedes cancer cell migration beginning at 6 hours post-treatment, coinciding with the evident reduction in pro-invasion gene expression, and before any alterations in the cell cycle or overall global protein synthesis are observed[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
MIA PaCa-2 1-100 nM Cell Viability Assay 72 h inhibits cell viability dose dependently 24971544
PANC-1 1-100 nM Cell Viability Assay 72 h inhibits cell viability dose dependently 24971544
PANC-1 50 nM Cell Viability Assay 24-96 h inhibits cell viability time dependently 24971544
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.23mL

0.65mL

0.32mL

16.16mL

3.23mL

1.62mL

32.33mL

6.47mL

3.23mL
参考文献

[1]Liu A, et al. mTOR Mediated Anti-Cancer Drug Discovery. Drug Discovery Today: Therapeutic Strategies. 2009, 6(2), 47-55.

[2]Hsieh AC, et al. The translational landscape of mTOR signalling steers cancer initiation and metastasis. Nature. 2012 Feb 22;485(7396):55-61.