AG-14361

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AG-14361

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Cat No: 24677

Biochemicals - Small Molecule Inhibitors

AG-14361 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1; Ki = 6.3 nM for the human enzyme).{43030} It inhibits PARP1 activity in permeabilized and intact SW620 cells (IC50s = 29 and 14 nM, respectively).{43031} AG-14361 (0.4 µM) potentiates t...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro-imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one

Correlated keywords:

AG14361 PARP-1 SW-620 A-2480 CP-70 HCT-116

Product Overview:
AG-14361 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1; Ki = 6.3 nM for the human enzyme).{43030} It inhibits PARP1 activity in permeabilized and intact SW620 cells (IC50s = 29 and 14 nM, respectively).{43031} AG-14361 (0.4 µM) potentiates the growth inhibitory effects of temozolomide (Item No. 14163) in HCT116, A2480, and CP70 cells and of the topoisomerase I inhibitor topotecan (Item No. 14129) by greater than three-fold in PARP1+/+ primary embryonic fibroblasts.{43032,43033} It slows the rejoining of camptothecin-induced DNA strand breaks.{43033} AG-14361 also inhibits cell growth in a PARP1-independent manner with GI50 values of 66 and 65 µM, respectively, in cell lines derived from PARP1+/+ and PARP1-/- mice.{43031} AG-14361 (15 mg/kg), in combination with temozolomide, leads to tumor regression in an SW620 mouse xenograft model.

Size	1 mg
Shipping	dry ice
CAS Number	328543-09-5
Molecular Formula	C₁₉H₂₀N₄O
SMILES	O=C1NCCN2C3=C1C=CC=C3N=C2C4=CC=C(CN(C)C)C=C4
Molecular Weight	320,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2924.19
UNSPSC code	12352100

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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.