Naquotinib

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Naquotinib

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Cat No: 23498

Biochemicals - Kinase Inhibitors

Naquotinib is an irreversible inhibitor of mutant EGF receptors (EGFRs).{36679} It inhibits proliferation of Ba/F3 cells expressing various EGFR mutations, including deletion of exon 19, deletion of exon 19 plus a T790M mutation, L858R, and L858R plus...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

6-ethyl-3-[[4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[[(3R)-1-(1-oxo-2-propen-1-yl)-3-pyrrolidinyl]oxy]-2-pyrazinecarboxamide

Correlated keywords:

F-3 T-790-M L-858-R C-797-S PC9 NaqRc-2 ASP8273 ASP-8273

Product Overview:
Naquotinib is an irreversible inhibitor of mutant EGF receptors (EGFRs).{36679} It inhibits proliferation of Ba/F3 cells expressing various EGFR mutations, including deletion of exon 19, deletion of exon 19 plus a T790M mutation, L858R, and L858R plus the T790M mutation (IC50s = 9, 10, 11, and 9 nM, respectively). It is selective for these mutations over the triple mutations that include exon 19 deletion plus T790M and C797S and L858R plus T790M and C797S and over wild-type EGFR (IC50s = 235, 1,994, and 830 nM, respectively). It reduces phosphorylated levels of EGFR, AKT, and ERK and decreases cell viability in non-small cell lung cancer (NSCLC) cells and in Ba/F3 cells carrying an exon 20 insertion mutation. Naquotinib (50 mg/kg per day) also reduces tumor growth in a PC-9/NaqRc2 mouse xenograft model.{36680}

Size	1 mg
Shipping	dry ice
CAS Number	1448232-80-1
Molecular Formula	C₃₀H₄₂N₈O₃
SMILES	CN1CCN(C2CCN(C3=CC=C(NC4=NC(O[C@H]5CN(C(C=C)=O)CC5)=C(CC)N=C4C(N)=O)C=C3)CC2)CC1
Molecular Weight	562,7
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.59
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.