Regorafenib

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Regorafenib

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Cat No: 18498

Biochemicals - Kinase Inhibitors

Regorafenib is an orally bioavailable multi-kinase inhibitor with anticancer activity.{29730} It inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ with IC50 values of 1.5, 2.5, 4.2, 7, 13, and 22 nM, respectively. Regorafenib also inhibits B-RAF,...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide

Correlated keywords:

1019206-88-2 755037-03-7 BAY 73-4506 734506 BAY734506 multikinase c-RAF BRAF VEGFR1 VEGFR2 VEGFR3 Tie2 PDGFR? FGFR1 c-Kit RET cRAF VEGFR-1 VEGFR-2 VEGFR-3 Tie-2 PDGFR-? FGFR-1 cKit epoxide hydrolase fluoro-sorafenib fluorosorafenib stivarga sEH PDGFRb PDGFR-b

Product Overview:
Regorafenib is an orally bioavailable multi-kinase inhibitor with anticancer activity.{29730} It inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ with IC50 values of 1.5, 2.5, 4.2, 7, 13, and 22 nM, respectively. Regorafenib also inhibits B-RAF, VEGFR3, FGFR, and Tie2 (IC50s = 28, 46, 202, and 311 nM, respectivey) as well as other kinases.{29730,27528,29728} In vivo, regorafenib (10 mg/kg) reduces tumor size in the MDA-MB-231 breast and 786-O renal cancer mouse xenograft models.{29730} It also reduces tumor microvessel area and inhibits tumor growth in a panel of mouse xenograft models. Formulations containing regorafenib have been used in the treatment of advanced gastrointestinal stromal tumors and metastatic colorectal cancer.

Size	5 mg
Shipping	dry ice
CAS Number	755037-03-7
Molecular Formula	C₂₁H₁₅ClF₄N₄O₃
SMILES	O=C(NC)C1=CC(OC2=CC=C(NC(NC3=CC(C(F)(F)F)=C(Cl)C=C3)=O)C(F)=C2)=CC=N1
Molecular Weight	482,8
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2922.19
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.