JAK2抑制剂V，Z3是可渗透细胞的吡啶基丁酮化合物，可同时抑制JAK2和活性V167F突变细胞自磷酸化。在无细胞激酶测定中，JAK2抑制剂V，Z3对COS细胞或SRC中的细胞Tyk 2自磷酸化没有作用。JAK2抑制剂V，Z3通过阻止G1-S过渡来抑制红白血病细胞系HEL的JAK2-V167F依赖性增殖，并显示可有效减少细胞因子刺激的Jak2-V617F阳性和Jak2-F537I阳性的生长骨髓增生异常患者的原代造血祖细胞。 JAK2 Inhibitor V, Z3 is a cell-permeable pyridinylbutanone compound that inhibits both JAK2 and the active V167F mutant cellular autophosphorylation. JAK2 Inhibitor V, Z3 displays no effect against cellular Tyk 2 autophosphorylation in COS cells or SRC in cell-free kinase assays. JAK2 Inhibitor V, Z3 suppresses the JAK2-V167F-dependent proliferation of the erythroleukemia cell line HEL by blocking the G1-S transition and is shown to effectively reduce the cytokine-stimulated growth of both Jak2-V617F-positive and Jak2-F537I-positive primary hematopoietic progenitor cells from myeloproliferative disorder patients.
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JAK2 Inhibitor V, Z3
CAS number：195371-52-9 molecular formula：C23H24N2O
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| Chinese alias | 2-甲基-1-苯基-4-吡啶-2-基-2-(2-吡啶-2-基)乙基)丁酮 | ||
| English alias | S6524 | SMR001527222 | A14132 | BCP06498 | DTXSID40285798 | JAK2 Inhibitor V | HMS3092H09 | 2-methyl-1-phenyl-4-(pyridin-2-yl)-2-(2-(pyridin-2-yl)ethyl)butan-1-one | 2-methyl-1-phenyl-4-pyridin-2-yl-2-(2-pyridin-2-ylethyl)butan-1-one | AC-35221 | VHA37152 | ||
| CAS number | 195371-52-9 | molecular formula | C23H24N2O |
| molecular weight | 344.5 g/mol | Exact mass | ≥98% |
| PSA | 42.900 Ų | logp | 4.500 |
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