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| Replacement Information |
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| Empirical Formula | CAS # |
|---|---|
| C₁₈H₁₆FN₃O | 457081-03-7 |
| Description | |
|---|---|
| Overview | A potent, reversible, cell-permeable, and ATP-competitive inhibitor of Janus protein tyrosine kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC50 = 15 nM for murine JAK1), JAK2 (IC50 = 1 nM), JAK3 (Ki = 5 nM), and Tyk2 (IC50 = 1 nM). Inhibits other kinases at much higher concentrations. Shown to inhibit IL2- and IL4-dependent proliferation of CTLL cells and block the phosphorylation of STAT5; and further induce growth inhibition of multiple myeloma cells expressing activated JAKs and STAT3, unlike AG 490 (Cat. No. 658401). A 10 mM (500 µg/162 µl) solution of JAK Inhibitor I (Cat. No. 420097) in DMSO is also available. |
| Catalogue Number | 420099 |
| Brand Family | Calbiochem® |
| Synonyms | 2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, Pyridone 6, P6, DBI, JAK1 Inhibitor I, JAK2 Inhibitor I, JAK3 Inhibitor X |
| References | |
|---|---|
| References | Pedranzini, L., et al. 2006. Cancer Res. 66, 9714. Lucet, I.S., et al. 2005. Blood 107, 176. Thompson, J.E., et al. 2002. Bioorg. Med. Chem. Lett. 12, 1219. |
| Product Information | |
|---|---|
| CAS number | 457081-03-7 |
| ATP Competitive | Y |
| Form | Off-white solid |
| Hill Formula | C₁₈H₁₆FN₃O |
| Chemical formula | C₁₈H₁₆FN₃O |
| Reversible | Y |
| Structure formula Image | |
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| Physicochemical Information | |
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| Cell permeable | Y |
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| Packaging Information | |
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| Packaged under inert gas | Packaged under inert gas |
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