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TG101348 is a JAK2 inhibitor (IC50 = 3 nM for wild-type and JAK2V617F enzymes).{61888} It is 35-, 334-, and 135-fold selective for JAK2 over JAK1, JAK3, and tyrosine kinase 2 (TYK2), respectively. It is also selective for JAK2 over a panel of 34 kinases at 500 nM but does inhibit FMS-related tyrosine kinase 3 (FLT3) and RET (IC50s = 15 and 48 nM, respectively). TG101348 reduces the proliferation of HEL human erythroleukemic cells as well as Ba/F3 murine hematopoioetic cells expressing JAK2V617F (IC50s = 305 and 270 nM, respectively). It inhibits the differentiation of hematopoietic stem cells and myeloid progenitor cells isolated from patients with the myeloproliferative neoplasm (MPN) polycythemia vera when used at a concentration of 300 nM.{61889} TG101348 (60 and 120 mg/kg) improves survival and reduces spleen weight in a syngeneic mouse model of polycythemia vera induced by transplantation of Jak2V617F-expressing whole bone marrow.{61888}
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 mg, 10 mg, 25 mg, 5 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 936091-26-8 |
| Molecular formula | C27H36N6O3S |
| Smiles | CC(C)(C)NS(C1=CC=CC(NC2=NC(NC3=CC=C(OCCN4CCCC4)C=C3)=NC=C2C)=C1)(=O)=O |
| Molecular weight | 524,7 |
| Custom code | 2933.59 |
| 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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