E7449 - CAS 1140964-99-3
Catalog number: 1140964-99-3
Category: Inhibitor
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Molecular Formula:
C18H15N5O
Molecular Weight:
317.34
COA:
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Targets:
PARP
Description:
E7449 is an orally bioavailable, potent, small molecule inhibitor of PARP1 and PARP2, which enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors.
Purity:
>98%
Synonyms:
E7449; E 7449; E-7449; 2X-121; 2X 121; 2X121;
MSDS:
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InChIKey:
JLFSBHQQXIAQEC-UHFFFAOYSA-N
InChI:
InChI=1S/C18H15N5O/c24-18-13-6-3-7-14-16(13)17(21-22-18)20-15(19-14)10-23-8-11-4-1-2-5-12(11)9-23/h1-7H,8-10H2,(H,22,24)(H,19,20,21)
Canonical SMILES:
C1C2=CC=CC=C2CN1CC3=NC4=CC=CC5=C4C(=N3)NNC5=O
1.E7449: A dual inhibitor of PARP1/2 and tankyrase1/2 inhibits growth of DNA repair deficient tumors and antagonizes Wnt signaling.
McGonigle S1, Chen Z1, Wu J1, Chang P2,3, Kolber-Simonds D1, Ackermann K1, Twine NC1, Shie JL1, Miu JT1,4, Huang KC1, Moniz GA5,6, Nomoto K1. Oncotarget. 2015 Dec 1;6(38):41307-23. doi: 10.18632/oncotarget.5846.
Inhibition of Poly(ADP-ribose) Polymerase1 (PARP1) impairs DNA damage repair, and early generation PARP1/2 inhibitors (olaparib, niraparib, etc.) have demonstrated clinical proof of concept for cancer treatment. Here, we describe the development of the novel PARP inhibitor E7449, a potent PARP1/2 inhibitor that also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1 and 2), important regulators of canonical Wnt/β-catenin signaling. E7449 inhibits PARP enzymatic activity and additionally traps PARP1 onto damaged DNA; a mechanism previously shown to augment cytotoxicity. Cells deficient in DNA repair pathways beyond homologous recombination were sensitive to E7449 treatment. Chemotherapy was potentiated by E7449 and single agent had significant antitumor activity in BRCA-deficient xenografts. Additionally, E7449 inhibited Wnt/β-catenin signaling in colon cancer cell lines, likely through TNKS inhibition. Consistent with this possibility, E7449 stabilized axin and TNKS proteins resulting in β-catenin de-stabilization and significantly altered expression of Wnt target genes.
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CAS 1140964-99-3 E7449

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