PF-299804

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PF-299804

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Cat No: 9001879

Biochemicals - Kinase Inhibitors

The epidermal growth factor receptors (EGFR), whose members include ErbB1 (HER1), ErbB2 (HER2), ErbB3 (HER3), and ErbB4 (HER4), are receptor tyrosine kinases that are often over-expressed in cancer.{17857,18353} PF-299804 is a second generation pan-Erb...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N-[4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-(2E)-butenamide

Correlated keywords:

1042385-75-0 epidermal growth factor receptors EGFR pan-erbB receptor tyrosine kinase RTK erbB-1 erbB-2 HER2 erbB-4 HER4 antitumor cancer inhibitor inhibit biochemical erbB1 erbB2 erbB4 HER 1 2 4 expression bind ATP adenosine triphosphate site catalytic domain growth regression xenograft model wild-type mutant family first generation second resistance resistant PF 00299804-03

Product Overview:
The epidermal growth factor receptors (EGFR), whose members include ErbB1 (HER1), ErbB2 (HER2), ErbB3 (HER3), and ErbB4 (HER4), are receptor tyrosine kinases that are often over-expressed in cancer.{17857,18353} PF-299804 is a second generation pan-ErbB receptor tyrosine kinase inhibitor (IC50s = 6, 45.7, and 73.7 nM for ErbB1, ErbB2, and ErbB4, respectively) that irreversibly binds to the ATP site in the catalytic domains of ErbB receptors.{27742,27743} At 15 mg/kg, it demonstrates antitumor activity ranging from delay in tumor growth to complete regression in various tumor xenograft models expressing either wild-type ErbB or mutant ErbB family members that show resistance to first generation ErbB kinase inhibitors.{27742,27743}

Size	1 mg
Shipping	dry ice
CAS Number	1110813-31-4
Molecular Formula	C₂₄H₂₅ClFN₅O₂
SMILES	O=C(NC1=C(OC)C=C(N=CN=C2NC3=CC(Cl)=C(F)C=C3)C2=C1)/C=C/CN4CCCCC4
Molecular Weight	469,9
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2903.99
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.