TX-1918 – CAS 503473-32-3 – Calbiochem

Descrição detalhada : A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K (IC50 = 440 nM), while it inhibits other kinases at much higher concentrations (IC50 = 4.4, 44, 44, and 440 microM for Src, PKA, PKC, and EGFR-K, respectively). Displays potent antitumor activity (EC50 = 2.07 and 230 microM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥5000-fold) and hepato-toxicity (≥90-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). It is therefore a more promising candidate as a therapeutic agent for cancer treatment., A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K (IC50 = 440 nM). Inhibits other kinases at much higher concentrations (IC50 = 4.4, 44, 44, and 440 microM for Src, PKA, PKC, and EGFR-K, respectively). Reported to exhibit potent anti-tumor activity (EC50 = 2.07 and 230 microM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥5000-fold) and hepato-toxicity (≥90-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). May be useful as a therapeutic agent for cancer treatment in animal models.
Sinónimos : TX-1918 - CAS 503473-32-3 - Calbiochem; 2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione
Fórmula molecula r: C14H12O3
Armazenamento : 2-8C; 2-8C; 2-8C
Embalagem : 1X10MG