Desmethyl Erlotinib

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Desmethyl Erlotinib

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Cat No: 23394

Biochemicals - Kinase Inhibitors

Desmethyl erlotinib is a metabolite of erlotinib (Item No. 10483).{40416} Erlotinib is a tyrosine kinase inhibitor which acts on the epidermal growth factor receptor (EGFR), inhibiting EGFR-associated kinase activity (IC50 = 2.5 µM).{18354,18362} This...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

2-[[4-[(3-ethynylphenyl)amino]-7-(2-methoxyethoxy)-6-quinazolinyl]oxy]-ethanol

Correlated keywords:

CP473420 OSI420 CP473,420 473420 JAK-2 HN-5 cdk nonsmall

Product Overview:
Desmethyl erlotinib is a metabolite of erlotinib (Item No. 10483).{40416} Erlotinib is a tyrosine kinase inhibitor which acts on the epidermal growth factor receptor (EGFR), inhibiting EGFR-associated kinase activity (IC50 = 2.5 µM).{18354,18362} This inhibits tumor growth in human head and neck carcinoma HN5 tumor xenografts in mice with an ED50 value of 9 mg/kg.{18354} Erlotinib also suppresses cyclin-dependent kinase 2 (Cdk2) activity in breast cancer cells (IC50 = 4.6 µM) and JAK2 mutant JAK2V617F positive hematopoietic progenitor cells (IC50 = 5 µM), which is associated with polycythemia vera, idiopathic myelofibrosis, and essential thrombocythemia.{16061,18355} Formulations containing erlotinib have been used to treat certain forms of cancer, including non-small cell lung cancer.{18351,17857}

Size	1 mg
Shipping	dry ice
CAS Number	183321-86-0
Molecular Formula	C₂₁H₂₁N₃O₄
SMILES	C#CC1=CC(NC2=NC=NC3=CC(OCCOC)=C(OCCO)C=C32)=CC=C1
Molecular Weight	379,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2921.30
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.