Ripretinib

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Ripretinib

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Cat No: 33782

Biochemicals - Kinase Inhibitors

Ripretinib is an inhibitor of KIT and PDGFRα (IC50s = 3 and 3.6 nM, respectively).{53053} It is selective for KIT and PDGFRα over a panel of 300 kinases (IC50s = >100 nM) but does inhibit DDR2, VEGFR2, PDGFRβ, and Tie2 (IC50s = V654A, KITT670I, KITD81...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N-[4-bromo-5-[1-ethyl-1,2-dihydro-7-(methylamino)-2-oxo-1,6-naphthyridin-3-yl]-2-fluorophenyl]-N?-phenyl-urea

Correlated keywords:

DCC2618 DP2618 DP-2618 Qinlock PDGFR-? ? VEGFR DDR-2 Tie-2 KIT-V654A T670I D816H D816V D842V 509I

Product Overview:
Ripretinib is an inhibitor of KIT and PDGFRα (IC50s = 3 and 3.6 nM, respectively).{53053} It is selective for KIT and PDGFRα over a panel of 300 kinases (IC50s = >100 nM) but does inhibit DDR2, VEGFR2, PDGFRβ, and Tie2 (IC50s = V654A, KITT670I, KITD816H, KITD816V, and PDGFRαD842V (IC50s = 11, 9.2, 18, 25, and 36 nM, respectively). Ripretinib induces apoptosis in ROSA wild-type, and KITD816V- or KITK509I-expressing mast cells in a concentration-dependent manner.{53054} It reduces tumor growth and increases survival in an imatinib-resistant patient-derived xenograft (PDX) mouse model of gastrointestinal stromal tumors (GISTs) when administered at doses of 50 and 100 mg/kg.{53053} Formulations containing ripretinib have been used in the treatment of GISTs.

Size	5 mg
Shipping	dry ice
CAS Number	1442472-39-0
Molecular Formula	C₂₄H₂₁BrFN₅O₂
SMILES	O=C(NC1=C(F)C=C(Br)C(C2=CC3=C(N(CC)C2=O)C=C(NC)N=C3)=C1)NC4=CC=CC=C4
Molecular Weight	510,4
Formulation	A solid
Purity	≥95%
Custom Code	2933.79
UNSPSC code	12352100

Technical File

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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.