Price of INK-128(MLN-0128)
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Technical DataFormula: C15H15N7O
Solubility : DMSO
Storage Conditions :Room temperature, or -20ºC for 2 year.
INK-128 MSDS INK-128 CoA
ReferenceThe translational landscape of mTOR signalling steers cancer initiation and metastasis
The mammalian target of rapamycin (mTOR) kinase is a master regulator of protein synthesis that couples nutrient sensing to cell growth and cancer. However, the downstream translationally regulated nodes of gene expression that may direct cancer development are poorly characterized. Using ribosome profiling, we uncover specialized translation of the prostate cancer genome by oncogenic mTOR signalling, revealing a remarkably specific repertoire of genes involved in cell proliferation, metabolism and invasion. We extend these findings by functionally characterizing a class of translationally controlled pro-invasion messenger RNAs that we show direct prostate cancer invasion and metastasis downstream of oncogenic mTOR signalling. Furthermore, we develop a clinically relevant ATP site inhibitor of mTOR, INK128, which reprograms this gene expression signature with therapeutic benefit for prostate cancer metastasis, for which there is presently no cure. Together, these findings extend our understanding of how the ¡®cancerous¡¯ translation machinery steers specific cancer cell behaviours, including metastasis, and may be therapeutically targeted.
Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment
C Garc¨ªa-Echeverr¨ªa - Bioorganic & medicinal chemistry letters, 2010 - Elsevier
... d]pyrimidine-2,4-diamine derivatives. View Within Article. AZD8055, AZD2014, OSI-027 and INK-128 have been the first optimized ATP-competitive mTOR inhibitors to enter clinical trials. Although most of the structures of these ...
[CITATION] INK128 is a potent and selective TORC1/2 inhibitor with broad oral antitumor activity
K Jessen, S Wang, L Kessler, X Guo, J Kucharski¡ - Mol Cancer Ther, 2009
Dual Targeting of -TORC1 and -TORC2 as a New Strategy In the Treatment of Multiple Myeloma
ASH Annual Meeting Abstracts 2010 116:133
INK128, a novel, potent, selective and orally...negative for this protein. We found that INK128 and rapamycin effectively suppressed phosphorylation of p6SR, but only INK128 was able to decrease phosphorylation...