CCT244747

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CCT244747

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Cat No: 25666

Biochemicals - Kinase Inhibitors

CCT244747 is a potent inhibitor of checkpoint kinase 1 (Chk1; IC50 = 8 nM).{41934} It is selective for Chk1 over FLT3, Chk2, and CDK1 (IC50s = 600, >10,000, and >10,000 nM, respectively) as well as a panel of 121 additional kinases at a concentration ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

3-[(1R)-2-(dimethylamino)-1-methylethoxy]-5-[[4-methoxy-5-(1-methyl-1H-pyrazol-4-yl)-2-pyridinyl]amino]-2-pyrazinecarbonitrile

Correlated keywords:

CCT-244747 Chk-1 2 CDK FLT-3 HT29 SW-620 MiaPaCa2 Calu6

Product Overview:
CCT244747 is a potent inhibitor of checkpoint kinase 1 (Chk1; IC50 = 8 nM).{41934} It is selective for Chk1 over FLT3, Chk2, and CDK1 (IC50s = 600, >10,000, and >10,000 nM, respectively) as well as a panel of 121 additional kinases at a concentration of 10 μM. CCT244747 reverses cell cycle arrest at the G2/M phase induced by etoposide (Item No. 12092) and SN-38 (Item No. 15632) in HT-29 cells and gemcitabine (Item Nos. 11690
9003096) in SW620 cells, indicating cellular G2 checkpoint abrogation. It potentiates the genotoxicity of SN-38, gemcitabine, and etoposide in HT-29, SW620, MiaPaCa-2, and Calu-6 cells with potentiation index (PI) values ranging from 1.9-8.5, 2.6-12.2, 5-16, and 1.4-5.6, respectively. In vivo, CCT244747 (75 mg/kg), in combination with irinotecan (Item No. 14180) or gemcitabine, increases the delay of tumor growth in SW620 and Calu-6 mouse xenograft models, respectively.

Size	1 mg
Shipping	dry ice
CAS Number	1404095-34-6
Molecular Formula	C₂₀H₂₄N₈O₂
SMILES	COC1=C(C2=CN(C)N=C2)C=NC(NC3=CN=C(C#N)C(O[C@H](C)CN(C)C)=N3)=C1
Molecular Weight	408,5
Formulation	A solid
Purity	≥98%
Custom Code	2933.39
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.

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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.