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Chemical Structure : E7449
CAS No.: 1140964-99-3
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).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $98 | In stock | |
| 10 mg | $148 | In stock | |
| 25 mg | $258 | In stock | |
| 50 mg | $398 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 317.3446 | |
| Formula | C18H15N5O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: < 6.96 mg/mL |
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| Chemical Name/SMILES |
3H-Pyridazino[3,4,5-de]quinazolin-3-one, 8-[(1,3-dihydro-2H-isoindol-2-yl)methyl]-1,2-dihydro- |
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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
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