An inhibitor of PARP1

E7449 – 25 mg

Brand:
Cayman
CAS:
1140964-99-3
Storage:
-20
UN-No:
Non-Hazardous - /

E7449 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 1 and 1.2 nM, respectively) as well as tankyrase (TNKS) 1/2 (IC50s = 50-100 nM).{42154} It is selective for PARP1, PARP2, and TNKS1/2 over PARP3 and PARP6-15 (IC50s = >3 μM). E7449 binds to chromatin in a concentration-dependent manner and inhibits growth of DT40 cells in a PARP-dependent manner (IC50s = 3.2 and >15 μM for wild-type and PARP-/- cells, respectively). It also decreases expression of the Wnt/β-catenin signaling pathway proteins axin2, total and active β-catenin, and cyclin D1 in SW480 cells. In vivo, E7449 enhances tumor growth inhibition induced by temozolomide (TMZ; Item No. 14163) in a B16/F10 isograft model as well as antitumor activity of the DNA-crosslinking agent carboplatin (Item No. 13112) in an MX-1 mouse xenograft model. E7449 (30 and 100 mg/kg per day) inhibits tumor growth in a BRCA1 mutant MDA-MB-436 breast cancer mouse xenograft model and induces complete inhibition of tumor cell PARP activity in an NCI-H460 lung cancer mouse xenograft model when administered at a dose of 100 mg/kg. It also delays hair regrowth, a TNKS-dependent process, in mice following hair removal.  

 

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Description

An inhibitor of PARP1, PARP2, and TNKS1/2 (IC50s = 1, 1.2, and 50-11 nM, respectively); selective for PARP1, PARP2, and TNKS1/2 over PARP3 and PARP6-15 (IC50s = >3 μM); inhibits growth of DT40 cells in a PARP-dependent manner (IC50s = 3.2 and >15 μM for wild-type and PARP-/- cells, respectively); decreases expression of Wnt/β-catenin signaling pathway proteins in SW480 cells; enhances antitumor activity of temozolomide and carboplatin in a B16/F10 isograft model and MX-1 mouse xenograft model, respectively; inhibits tumor growth in a BRCA1 mutant MDA-MB-436 breast cancer mouse xenograft model at 30 and 100 mg/kg per day; delays hair regrowth in mice following hair removal,

Formal name: 8-[(1,3-dihydro-2H-isoindol-2-yl)methyl]-1,2-dihydro-3H-pyridazino[3,4,5-de]quinazolin-3-one

Synonyms: 

Molecular weight: 317.3

CAS: 1140964-99-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|DNA Repair Enzymes||Research Area|Cancer|DNA Damage and Repair|PARP||Research Area|Cell Biology|Cell Signaling|Wnt Signaling||Research Area|Epigenetics, Transcription, & Translation|RNA, DNA, & Protein Synthesis

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