ON-123300

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ON-123300

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Cat No: 19902

Biochemicals - Kinase Inhibitors

ON-123300 is a multi-kinase inhibitor.{43515,43516} It inhibits ARK5, Cdk4, and Cdk6 (IC50s = 3.87, 9.82, and 4.95 nM, respectively) as well as FYN, PDGFRβ, Abl, and PI3Kδ (IC50s = 11.09, 26, 53.32, and 144 nM, respectively) among others.{43516} It in...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

8-cyclopentyl-7,8-dihydro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-7-oxo-pyrido[2,3-d]pyrimidine-6-carbonitrile

Correlated keywords:

ON123300 CDK4 Ark-5 PDGFR-? FGFR1 PI3K-? u-87 G2-M MDAMB MB231 MDAMB231 cdk-4-6 multikinase G-2 U87VIII U87PTEN

Product Overview:
ON-123300 is a multi-kinase inhibitor.{43515,43516} It inhibits ARK5, Cdk4, and Cdk6 (IC50s = 3.87, 9.82, and 4.95 nM, respectively) as well as FYN, PDGFRβ, Abl, and PI3Kδ (IC50s = 11.09, 26, 53.32, and 144 nM, respectively) among others.{43516} It inhibits proliferation in a panel of 38 cancer cell lines (GI50s = 0.05-5 µM).{43516} ON-123300 also inhibits proliferation of U87 glioma cells (IC50 = 3.4 µM), decreases phosphorylation of Akt and activates ERK, as well as halts the cell cycle in the G2/M phase and induces apoptosis.{43515} When used in combination with the EGFR inhibitor gefitinib (Item No. 13166), it synergistically induces cytotoxicity of U87, U87 VIII, and U87 PTEN cells. ON-123300 reduces tumor growth in an MDA-MB-231 mouse xenograft model when administered at a dose of 50 mg/kg every other day.{43516}

Size	1 mg
Shipping	dry ice
CAS Number	1357470-29-1
Molecular Formula	C₂₄H₂₇N₇O
SMILES	CN1CCN(C2=CC=C(NC3=NC(N(C4CCCC4)C(C(C#N)=C5)=O)=C5C=N3)C=C2)CC1
Molecular Weight	429,5
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.49
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.