E7449

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E7449

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Cat No: 21658

Biochemicals - Small Molecule Inhibitors

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...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

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

Correlated keywords:

E-7449 PARP-1 2 3 6 PARP15 TNKS-1 TNKS2 DT-40 SW-480 B-16 F-10 MX1 BRCA-1 axin-2 MDAMB-436 anti-tumor NCIH460 MDAMB436

Product Overview:
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.

Size	1 mg
Shipping	dry ice
CAS Number	1140964-99-3
Molecular Formula	C₁₈H₁₅N₅O
SMILES	O=C1C2=CC=CC3=C2C(N=C(CN4CC(C=CC=C5)=C5C4)N3)=NN1
Molecular Weight	317,3
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2928.00
UNSPSC code	12352100

Technical File

MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.