Defactinib

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Defactinib

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Cat No: 17737

Biochemicals - Kinase Inhibitors

Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that plays a vital role in many oncogenic pathways.{28867,28866} Defactinib is a dose-dependent inhibitor of FAK, with maximal inhibition of FAK autophosphorylation in cells achieved at 10 µ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N-?methyl-?4-?[[4-?[[[3-?[methyl(methylsulfon?yl)?amino]?-?2-?pyrazinyl]?methyl]?amino]?-?5-?(trifluoromethyl)?-?2-?pyrimidinyl]?amino]?-benzamide

Correlated keywords:

1073160-26-5 biochemical inhibitor cancer signal transduction intracellular signaling protein kinase inhibit VS6063 PF04554878 FAK focal adhesion

Product Overview:
Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that plays a vital role in many oncogenic pathways.{28867,28866} Defactinib is a dose-dependent inhibitor of FAK, with maximal inhibition of FAK autophosphorylation in cells achieved at 10 µM.{28865} It is less effective against the related kinase PYK2. Defactinib restores the chemosensitivity of taxane-resistant cells to paclitaxel (Item No. 10461), although it is not cytotoxic alone.{28865} Defactinib decreases YB-1 phosphorylation and nuclear accumulation in an Akt-dependent manner. It is orally bioavailable, inhibiting FAK and augmenting paclitaxel action in suppressing the growth and number of ovarian cancer cell tumors in mice.{28865}

Size	1 mg
Shipping	dry ice
CAS Number	1073154-85-4
Molecular Formula	C₂₀H₂₁F₃N₈O₃S
SMILES	O=C(NC)C1=CC=C(NC2=NC=C(C(F)(F)F)C(NCC3=NC=CN=C3N(C)S(C)(=O)=O)=N2)C=C1
Molecular Weight	510,5
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.