Catalog No.: PC-43025Not For Human Use, Lab Use Only.
E7449 (2X-121) is a potent, orally bioavailable, brain penetrable dual inhibitor of PARP1/2 and TNKS1/2 with IC50 of 2.0/1.0 nM (PARP1/2), 50-100 nM (TNKS1/2).
E7449 (Stenoparib, 2X-121) is a potent, orally bioavailable, brain penetrable dual inhibitor of PARP1/2 and TNKS1/2 with IC50 of 2.0/1.0 nM (PARP1/2), 50-100 nM (TNKS1/2).
E7449 (Stenoparib, 2X-121) displays no significant inhibitory activity for PARP3 or PARPs6-16.
E7449 (Stenoparib, 2X-121) shows sensitivity to cells deficient in DNA repair pathways beyond homologous recombination, inhibits Wnt/β-catenin signaling in colon cancer cell lines, stabilizes axin and TNKS proteins resulting in β-catenin de-stabilization and significantly alters expression of Wnt target genes.
E7449 (Stenoparib, 2X-121) potentiates antitumor activity of chemotherapies temozolomide and carboplatin both in vitro and in vivo.
1. McGonigle S, et al. Oncotarget. 2015 Dec 1;6(38):41307-23.
2. Sharon McGonigle, et al. Abstract 4688: E7449: A novel PARP inhibitor enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors . Cancer Research: April 15, 2012; Volume 72, Issue 8, Su
