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| | ON044580 Basic information |
| Product Name: | ON044580 | | Synonyms: | ON044580;Benzoic acid, 4-[(2E)-2-[[(4-bromophenyl)methyl]thio]-3-(4-fluoro-3-nitrophenyl)-1-oxo-2-propen-1-yl]- | | CAS: | 1035199-04-2 | | MF: | C23H15BrFNO5S | | MW: | 516.34 | | EINECS: | | | Product Categories: | | | Mol File: | 1035199-04-2.mol |  |
| | ON044580 Chemical Properties |
| Melting point | 170-172 °C(Solvent: Isopropanol) | | Boiling point | 701.806±60.00 °C(Press: 760.00 Torr)(predicted) | | density | 1.586±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | | pka | 3.723±0.10(predicted) |
| | ON044580 Usage And Synthesis |
| Uses | ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling[1]. | | IC 50 | JAK2-WT: 1.23 μM (IC50); JAK2-V617F: 1.09 μM (IC50); WT BCR-ABL; T315I-BCR-ABL | | References | [1] Shashidhar S Jatiani, et al. A Non-ATP-Competitive Dual Inhibitor of JAK2 and BCR-ABL Kinases: Elucidation of a Novel Therapeutic Spectrum Based on Substrate Competitive Inhibition. Genes Cancer. 2010 Apr;1(4):331-45. DOI:10.1177/1947601910371337 |
| | ON044580 Preparation Products And Raw materials |
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