ABT-869

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ABT-869

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Cat No: 13653

Biochemicals - Kinase Inhibitors

Receptor tyrosine kinases (RTKs) mediate critical signaling transduction pathways important for cell survival, growth, and differentiation. Whereas aberrant tyrosine kinase signaling is correlated with the progression of various cancers, RTK inhibitors...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N-[4-(3-amino-1H-indazol-4-yl)phenyl]-N’-(2-fluoro-5-methylphenyl)-urea

Correlated keywords:

ABT869 VEG PDG FR VEGFR 1 2 FLT 3 CSF1R cMet Tie 2 HT29 MDAMB435 MV411 MOLM13

Product Overview:
Receptor tyrosine kinases (RTKs) mediate critical signaling transduction pathways important for cell survival, growth, and differentiation. Whereas aberrant tyrosine kinase signaling is correlated with the progression of various cancers, RTK inhibitors are useful as cancer therapy agents. ABT-869 is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of the vascular endothelial growth factor (VEGF) and platelet derived growth factor (PDGF) receptor families (e.g., KDR, FLT1, FLT3, FLT4, CSF-1R, and KIT) demonstrating IC50 values ranging from 4-190 nM.{18810} ABT-869 shows little activity against unrelated RTKs, cytoplasmic tyrosine kinases, or Ser/Thr kinases (IC50s > 1 μM).{18810} ABT-869 inhibits proliferation in MV-4-11 and MOLM-13 cells (acute myeloid leukemia cell lines harboring RTK mutations; IC50s = 4 and 6 nM, respectively), inducing apoptosis as evidenced by an increased sub-G0/G1 phase cell population, caspase activation, and PARP cleavage.{18812} In murine xenograft models, as well as in a phase 1 clinical trial, ABT-869 demonstrated respectable efficacy in solid tumors including lung and hepatocellular carcinomas.{18811}

Size	1 mg
Shipping	dry ice
CAS Number	796967-16-3
Molecular Formula	C₂₁H₁₈FN₅O
SMILES	NC1=NNC2=C1C(C3=CC=C(NC(NC4=C(F)C=CC(C)=C4)=O)C=C3)=CC=C2
Molecular Weight	375,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.19
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.