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mTOR-IN-1_1207358-59-5_DataSheet_MedChemExpress

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Product Data Sheet

Product Name: CAS No.: Cat. No.: MWt: Formula: Purity :

mTOR-IN-1 1207358-59-5 HY-18353 474.56 C25H30N8O2 >98%

Solubility:

DMSO

Mechanisms: Pathways:PI3K/Akt/mTOR ; Target:mTOR Biological Activity: mTOR IN 1 is a potent and selective ATP-competitive ATP competitive inhibitor of mTOR with Ki of 1 1.5 nM. mTOR-IN-1 5 nM IC50 Value: 1.5 nM (Ki) Target: mTOR Selective inhibitors of mammalian target of rapamycin (mTOR) kinase based upon saturated heterocycles fused to a pyrimidine core were designed and synthesized. Each series produced compounds with Ki < 10 nM for the mTOR kinase and >500-fold selectivity over closely related PI3 kinases. This potency translated into strong pathway inhibition, as measured by phosphorylation of mTOR substrate proteins and antiproliferative activity in cell lines with a constitutively active PI3K pathway. Two compounds exhibiting suitable mouse PK were profiled in in vivo tumor models and were shown to suppress mTORC1 and mTORC2 signaling for over 12 h when dosed orally. Both compounds were additionally shown to suppress tumor growth in vivo in a PC3 prostate cancer...

References: [1]. Koehler, Michael F. T.; Bergeron, Philippe; Blackwood, Elizabeth et al. Potent, Selective, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin Kinase Domain Exhibiting Single g Agent g Antiproliferative p Activity. y Journal of Medicinal Chemistry y( (2012), ), 55(24), ( ), 10958-10971.

Caution: Not fully tested. For research purposes only Medchemexpress LLC

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