Gefitinib-based PROTAC 3

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Cat No: 28597

Biochemicals - More Biochemicals

Gefitinib-based PROTAC 3 is a proteolysis-targeting chimera (PROTAC) comprised of the EGF receptor (EGFR) inhibitor gefitinib (Item No. 13166) linked to the von Hippel-Lindau (VHL) E3 ubiquitin ligase ligand VHL ligand 1 (Item No. 21591).{52051} In ce...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

(2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)pentyl)oxy)ethoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

Correlated keywords:

PROTAC3 CC827 H3255 L858R L-858-R L858 858R CC-827 H-3255

Product Overview:
Gefitinib-based PROTAC 3 is a proteolysis-targeting chimera (PROTAC) comprised of the EGF receptor (EGFR) inhibitor gefitinib (Item No. 13166) linked to the von Hippel-Lindau (VHL) E3 ubiquitin ligase ligand VHL ligand 1 (Item No. 21591).{52051} In cell-based assays, gefitinib-based PROTAC 3 induces degradation of EGFR containing the activating mutation L858R or an exon 19 deletion with half-maximal degradation (DC50) values of 22.3 and 11.7 nM, respectively, but does not induce degradation of wild-type EGFR at concentrations up to 10 μM.

Size	1 mg
Shipping	dry ice
CAS Number	2230821-27-7
Molecular Formula	C₄₇H₅₇ClFN₇O₈S
SMILES	ClC1=CC(NC2=NC=NC3=C2C=C(OCCCCCOCCOCCC(N[C@@H](C(C)(C)C)C(N4C[C@H](O)C[C@H]4C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)C(OC)=C3)=CC=C1F
Molecular Weight	934,5
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2934.10
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.