CAS No. : 1062169-56-5

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000313
Synonyms:methyl 4-[6-[4-(methoxycarbonylamino)phenyl]-4-morpholin-4-ylpyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carboxylate
Molecular Formula:C24H29N7O5
Molecular Weight:495.5
IC50:5 nM [1]
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Appearance:Solid powder
Purity: > 98%
Cat No:I000313
Cas No:1062169-56-5

WYE-354 is a potent, specific and ATP-competitive inhibitor of mTOR with IC50 of 5 nM, blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) not P-AKT(T308), selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
IC50 value: 5 nM [1]
Target: mTOR
in vitro: WYE-354 also inhibits several PI3Ks at micromolar levels. In HEK293 cells, WYE-354 (0.2 μM–5 μM) effectively inhibits both mTORC1 and mTORC2. WYE-354 (0.3 μM–10 μM) significantly blocks mTOR signaling and Akt activation in U87MG and MDA361 cells. Furthermore, WYE-354 potently inhibits proliferation in tumor cell lines including MDA-MB-361, MDA-MB-231, MDA-MB-468, LNCap, A498, and HCT116, with IC50 values ranging from 0.28 μM to 2.3 μM. The apoptosis induced by WYE-354 is accompanied by G1 cell cycle arrest and caspases activation [1]. In endothelial HUVEC cells, WYE-354 (10 nM–1 μM) also inhibits both mTORC1 and mTORC2 signaling, as revealed by dephosphorylation of S6 ribosomal protein and Akt, respectively. Furthermore, WYE-354 (10 nM–1 μM) activates mitogen-activated protein kinase (MAPK) signaling, which may be due to its inhibition of mTORC1 [2].
in vivo: In a mice xenograft model of PTEN-null PC3MM2 tumor, WYE-354 (50 mg/kg) effectively inhibits mTOR signaling and tumor growth [1].

1:Autophagy inhibition sensitizes WYE-354-induced anti-colon cancer activity in vitro and in vivo. Wang L, Zhu YR, Wang S, Zhao S.Tumour Biol. 2016 Sep;37(9):11743-11752. Epub 2016 Mar 28. PMID: 27020593
2:Rapamycin and WYE-354 suppress human gallbladder cancer xenografts in mice. Weber H, Leal P, Stein S, Kunkel H, García P, Bizama C, Espinoza JA, Riquelme I, Nervi B, Araya JC, Grez M, Roa JC.Oncotarget. 2015 Oct 13;6(31):31877-88. doi: 10.18632/oncotarget.5047. PMID: 26397134 Free PMC Article
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