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AZD 9291 is an inhibitor of mutant EGFRs (IC50s = 1, 12, and 5 nM for EGFRL858R/T790M, EGFRL858R, and EGFRL861Q, respectively).{66077} It is selective for these mutant EGFRs over wild-type EGFR (IC50 = 184 nM), as well as over a panel of approximately 280 other kinases at 1 µM. AZD 9291 selectively inhibits the proliferation of mutant EGFR-containing non-small cell lung cancer (NSCLC) cells, including H1975 cells containing the L858R activating and T790M resistance mutations, PC-9 cells containing the activating exon 19 deletion, and vandetanib-resistant PC-9 cells, which contain the exon 19 deletion and T790M mutation (IC50s = 11, 8, and 40 nM, respectively), over wild-type EGFR-containing Calu-3 and NCI H2073 NSCLC cells (IC50s = 650 and 461 nM, respectively). It induces tumor regression in a vandetanib-resistant PC-9 mouse xenograft model when administered at doses ranging from 1 to 10 mg/kg. Formulations containing AZD 9291 have been used in the treatment of EGFR mutant-containing NSCLC.
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 mg, 10 mg, 5 mg, 50 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 1421373-65-0 |
| Molecular formula | C28H33N7O2 |
| Smiles | CN(CCN(C)C)C1=C(NC(C=C)=O)C=C(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)C(OC)=C1 |
| Molecular weight | 499,6 |
| Custom code | 2922.19 |
| Formulation | A crystalline solid |
| Purity | ≥98% |
| UNSPSC code | 12352100 |
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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