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Ilorasertib is a multi-kinase inhibitor.{62231} It inhibits Aurora C, VEGFR1, VEGFR2, FLT3, colony-stimulating factor 1 receptor (CSF1R), and Aurora B (IC50s = 1, 1, 2, 1, 3, and 7 nM, respectively). It also inhibits PDGFR?, PDGFR?, c-Kit, VEGFR3, and Aurora A (IC50s = 11, 13, 20, 43, and 120 nM, respectively). Ilorasertib inhibits autophosphorylation of Aurora A, -B, and -C in HeLa cells with IC50 values of 189, 13, and 13 nM, respectively. It inhibits proliferation of a variety of cancer cells, including MV4-11 acute myeloid leukemia (AML), SUP-B15 acute lymphocytic leukemia (ALL), and H1299 non-small cell lung cancer (NSCLC) cells (IC50s = 0.3, 4, and 2 nM, respectively). It decreases histone H3 phosphorylation in blood-borne tumor cells in an engrafted mouse model of leukemia when administered at a dose of 25 mg/kg and reduces tumor growth in fibrosarcoma, pancreatic carcinoma, ALL, and multiple myeloma mouse xenograft models.
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 mg, 10 mg, 25 mg, 5 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 1227939-82-3 |
| Molecular formula | C25H21FN6O2S |
| Smiles | O=C(NC1=CC(F)=CC=C1)NC2=CC=C(C3=CSC4=C(C5=CN(CCO)N=C5)C=NC(N)=C43)C=C2 |
| Molecular weight | 488,5 |
| Custom code | 2934.99 |
| Formulation | A 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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Amyloid-? (1-8, A2V) is a truncated form of amyloid-? (A?) that contains a valine to alanine substitution at position 2...
To be used in conjunction with Cayman’s NAPE-PLD polyclonal antibody (aa 6-20) (Item No. 10306) to block protein-antibody complex formation...
This mixture contains the characteristic metabolites of both PGI2 and TXA2. Contents: Thromboxane B2, 11-dehydro Thromboxane B2, 6-keto Prostaglandin F1?,...
Platelet-activating factor (PAF) is an important lipid mediator involved in inflammation. PAF-acetylhydrolase (PAF-AH) is an extracellular phospholipase A2 which hydrolyzes...
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Sirtuin 5 (SIRT5) is an enzyme that catalyzes the NAD-dependent removal of malonyl, succinyl, and glutaryl groups from target proteins.{55107,55108}...
The Cayman COX Inhibitor Pack contains a combination of frequently used cyclooxygenase (COX) inhibitors. Each kit contains aspirin, the archetype...
Programmed cell death protein 4 (PDCD4) levels are elevated during apoptosis and absent in many cancer samples.{16340,16167} Loss of PDCD4...
Proprotein convertase subtilisin kexin 9 (PCSK9) is a member of the subtilisin serine protease family with an important role in...
To be used in conjunction with Cayman’s FABP3 polyclonal antibody (Catalog No. 10233) to block protein-antibody complex formation during immunochemical...
Inositol hexakisphosphate kinase 2 (IP6K2) is a cytoplasmic kinase that catalyzes the conversion of IP6 to diphosphoinositol pentakisphosphate in the...
Protein phosphorylation is an important post-translational modification that serves many key functions to regulate a protein’s activity, localization, and protein-protein...
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