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Akt functions as a key component in multiple signaling pathways including those related to cell proliferation, metabolism, and survival as well as angiogenesis. AZD 5363 is a pyrrolopyrimidine-derived compound that inhibits Akt by competitively binding to the kinase domain, preventing substrate phosphorylation by Akt.{25455} It inhibits Akt1, 2, and 3 with IC50 values of 3, 7, and 7 nM, respectively and also inhibits P70S6K and PKA with similar potency (IC50s = 6 and 7 nM, respectively).{25455} Furthermore, AZD 5363 shows >75% inhibition at 1 ?M against ROCK2, MKK1, MSK1, MSK2, PKC?, PKG?, PKG?, PRKX, RSK2, and RSK3.{25455} At 3 ?M or less, AZD 5363 has been reported to inhibit the proliferation of 41 out of 182 solid and hematologic tumor cell lines, demonstrating the greatest sensitivity towards breast cancer derived-cells or those with PIK3CA and/or PTEN mutations.{25455} Oral dosing to nude mice bearing BT474c xenografts resulted in antitumor activity, including the reduction of the phosphorylation of PRAS40, GSK3?, and S6 at an EC50 value of ~ 0.1 ?M.{25455}
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 mg, 10 mg, 25 mg, 5 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 1143532-39-1 |
| Molecular formula | C21H25ClN6O2 |
| Smiles | O=C(N[C@@H](CCO)C1=CC=C(Cl)C=C1)C(CC2)(N)CCN2C3=C4C(NC=C4)=NC=N3 |
| Molecular weight | 428,9 |
| Custom code | 2933.39 |
| 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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