(4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile

(4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile 화학적 특성, 용도, 생산

• 개요

  BMS 214662 is a potent inhibitor of farnesyltransferase (FTase; IC₅₀ = 1.3 nM). It is selective for FTase over geranylgeranyl transferase (GGTase; IC₅₀ = 1,900 nM). It inhibits the growth of MEK2, A2780, and PC3 cancer cells expressing wild-type Ras (IC₅₀s = 2.5, 0.04, and 0.15 μM, respectively), as well as HCT116, MIP, RC-165, and MIA PaCa-2 cells expressing mutant K-Ras (IC₅₀s = 0.06, 0.3, 0.3, and 0.12 μM, respectively). BMS 214662 induces apoptosis in HCT116 cells in a concentration-dependent manner. In vivo, BMS 214662 (600 mg/kg) is curative in an HCT116 mouse xenograft model. It also reduces tumor growth in Calu-1, HT-29, EJ-1, and MIA PaCa-2 mouse xenograft models.

• 화학적 성질

  Pale Yellow Solid

• 용도

  A potent and selective inhibitor of farnesyltransferase that induces mitochondrial apoptosis in chronic myeloid leukemia stem/progenitor cells, including CD34+38- cells, through activation of protein kinase Cβ.

(4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile 공급 업체

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