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AST-487

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    AST-487
  • AST-487
Cat No: 19477
Biochemicals - Kinase Inhibitors
Cayman

AST-487 is an inhibitor of RET (IC50 = 0.88 µM), FLT3 (Ki = 0.52 µM), KDR (IC50 = 0.17 µM), c-Abl (IC50 = 0.02 µM), and c-Kit (IC50 = 0.5 µM).{31675,31676} It has been shown to inhibit RET autophosphorylation and activation of downstream effectors and...

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Territorial Availability: Available through Bertin Technologies only in France
Synonyms:
  • N-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-N'-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]-urea
Correlated keywords:
  • 1069112-48-6 AST487 NVPAST487 NVP-AST487 NVPAST-487 RET KDR c-Abl auto-phosphorylation NIH-3T3 MTC FLT3 c-Kit Fms tyrosine cAbl cKit FLT-3 FLT3ITD bearing internal-tandem duplication MTCTT anti-proliferative multikinase
Product Overview:
AST-487 is an inhibitor of RET (IC50 = 0.88 µM), FLT3 (Ki = 0.52 µM), KDR (IC50 = 0.17 µM), c-Abl (IC50 = 0.02 µM), and c-Kit (IC50 = 0.5 µM).{31675,31676} It has been shown to inhibit RET autophosphorylation and activation of downstream effectors and to prevent the growth of human thyroid cancer cell lines with activating mutations of RET but not of lines without RET mutations.{31675} In xenografts of NIH3T3 cells expressing oncogenic RET and of the MTC cell line TT in nude mice, AST-487 dose dependently inhibited tumor growth.{31675} It also demonstrates antiproliferative effects on primary cells from acute myelocytic leukemia patients and on cell lines expressing FLT3-ITD or FLT3 kinase domain point mutants.{31675}
Size 1 mg
Shipping dry ice
CAS Number 630124-46-8
Molecular Formula C26H30F3N7O2
SMILES CNC1=CC(OC2=CC=C(NC(NC3=CC=C(CN4CCN(CC)CC4)C(C(F)(F)F)=C3)=O)C=C2)=NC=N1
Molecular Weight 529,6
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.

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