WYE354

WYE354 価格

WYE354 化学特性,用途語,生産方法

• 説明

  WYE-354 is a potent cell-permeable inhibitor of mTOR (IC₅₀ = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2. It is a much weaker inhibitor of phosphatidylinositol 3-kinase α (IC₅₀ = 1,026 nM) and other kinases. WYE-354 induces G₁ cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines, inhibits mTORC1 and mTORC2 in tumor-bearing mice, and reduces tumor growth in nude mice with PTEN-null tumors.

• 使用

  A pyrazolopyrimidines derivative that is a potent and ATP-competitive mTOR inhibitor with much reduced activity against PI 3-Kα or PI 3-Kγ. WYE-354 is equally potent against mTORC1 and mTORC2 activities in HEK293 immune complex kinase assays using S6K and Akt as the respective substrate (IC50 <200 nM; [ATP] = 100 μM) and effectively blocks cellular phosphorylation of S6K on T389 and Akt on S473 both in cultures and in a murine xenograft model, resulting in a significant suppression of PC3MM2-derived tumor growth (by 86% on day 7; 50 mg/kg, i.p twice per day) in vivo.

WYE354 生産企業

Global(94)Suppliers

WYE354 スペクトルデータ(¹HNMR)

1062169-56-5, WYE354 キーワード