WYE-354

Short Summary : MTOR inhibitor,potent,ATP-competitive and cell-permeable

Category : PI3K/Akt/mTOR Signaling|mTOR

Purity : 0.9806

CAS Number : 1062169-56-5

Formula : C24H29N7O5

Molecular Weight : 495.53

SMILE : COC(=O)NC1=CC=C(C=C1)C2=NC3=C(C=NN3C4CCN(CC4)C(=O)OC)C(=N2)N5CCOCC5

Solubility : >49.6mg/mL in DMSO

Storage : Store at -20°C

Description : WYE-354 is a powerful and selective ATP-competitive kinase heterocyclic inhibitors with biochemical IC50 of 5 nM against mTOR.[1]WYE-354 displays very specific selectivity to PI3K families (>100-fold to PI3K and >500-fold to PI3K ), but it cant inhibit some protein kinases. May cancer cell lines including MDA-MB-468 and U87MG can be inhibited by WYE-354 in 0.3C1 mM range.[1]In-vitro study has proved that WYE-354 can inhibit substrate phosphorylation such as p-4E-BP1 T37/46 and p-Akt S473 by mTORC1 and mTORC2. WYE-354 can reduce Akt downstream function and block the propagation of the cancer cell lines with an IC50 value from sub-micromolar to micromolar range [3]. These effects were consistent with the G1 cell cycle arrest in two cell lines, including rapamycin-sensitive and rapamycin-resistant cells. It is believed to induce apoptosis, repress the global protein synthesis, and down-regulate many angiogenic factors.[3]References:[1] Qingsong Liu, Carson Thoreen, Jinhua Wang, David Sabatini, Nathanael S. Gray. mTOR mediated anti-cancer drug discovery. Drug Discovery Today. 2009. 6(2): 47-55.[2] Shi-Yong Sun. mTOR kinase inhibitors as potential cancer therapeutic drugs. Cancer Letters. 28 October 2013. 340(1): 1-8.

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