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  • 5 mg - 284 EUR
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  • 100 mg - 3408 EUR

WAY-600

WAY-600 is a single digit nanomolar inhibitor of the mTOR kinases, with significant selectivity for these enzymes over phosphatidylinositol 3-kinase (PI3K) isofoms (>100-fold). Both in vivo and in vitro, this compound is differentiated from the rapalogs in that is blocks substrate phosphorylation by mTORC1 and mTORC2 induced by growth factors, amino acids, and hyperactive PI3K/AKT. Unlike the inhibitors of PI3K or dual-pan PI3K/mTOR inhibitors, BAY-600 achieved cellular inhibition of P-S6K1(T389) and P-AKT(S473) at significantly lower inhibitor concentrations than were required to reduce P-AKT(T308) activity (as judged by the PI3K-PDK1 readout), demonstrating its mTOR selectivity. WAY-600 inhibited the activity of proteins downstream of AKT and the proliferation of diverse cancer cell lines. These effects correlated with a strong G(1) cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cells, selective induction of apoptosis, repression of global protein synthesis, and down-regulation of angiogenic factors.

catalogue number: W089
synonyms:
CAS: 1062159-35-6
MW: 494.59 g/mol

References
Cancer Res. 2009 Aug 1;69(15):6232-40. PMID: 19584280