TAS 0728

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TAS 0728

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Cat No: 33528

Biochemicals - Kinase Inhibitors

TAS 0728 is a covalent HER2 inhibitor (IC50 = 36 nM).{57578} It is selective for HER2 over panels of 386 and 374 additional kinases, as well as a panel of 68 non-kinase enzymes, when used at a concentration of 1 µM. TAS 0728 inhibits HER2 autophosphor...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

4-amino-N-[4-[2-(dimethylamino)-2-oxoethyl]-2,3-dimethylphenyl]-1-[(3R)-1-(1-oxo-2-propen-1-yl)-3-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide

Correlated keywords:

TAS0728 HER-2 nonkinase SKBR BR3 SKBR3 A-431 NCIN87 BT-474

Product Overview:
TAS 0728 is a covalent HER2 inhibitor (IC50 = 36 nM).{57578} It is selective for HER2 over panels of 386 and 374 additional kinases, as well as a panel of 68 non-kinase enzymes, when used at a concentration of 1 µM. TAS 0728 inhibits HER2 autophosphorylation in HER2-overexpressing SK-BR-3 cells but not autophosphorylation of EGFR in EGFR-overexpressing A431 cells. It inhibits the growth of six HER2-amplified breast, lung, and gastric cancer cell lines (GI50s = 1.6-31 nM). TAS 0278 (30 and 60 mg/kg) reduces tumor volume in NCI N87 and BT474 mouse xenograft models.

Size	1 mg
Shipping	dry ice
CAS Number	2088323-16-2
Molecular Formula	C₂₆H₃₂N₈O₃
SMILES	CC(C(C)=C(C=C1)CC(N(C)C)=O)=C1NC(C2=NN([C@@]3([H])CN(CCC3)C(C=C)=O)C4=NC=NC(N)=C42)=O
Molecular Weight	504,6
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.