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| 品牌 | absin | CAS | 540737-29-9 |
|---|---|---|---|
| 分子式 | C22H28N6O8 | 纯度 | ＞98% |
| 分子量 | 504.49 | 货号 | abs47028031 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | is a novel inhibitor of JAK3 | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Tofacitinib Citrate 540737-29-9
| 产品描述 | |
| 描述 | Tofacitinib citrate (CP-690550 citrate) is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1. |
| 纯度 | ＞98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 枸橼酸托法替尼；Tasocitinib citrate；CP-690550 citrate |
| 外观 | White to off-white powder |
| 可溶性/溶解性 | DMSO ：50.5 mg/mL (100 mM) |
| 生物活性 | |
| 靶点 | JAK3,JAK2 |
| In vitro(体外研究) | Tofacitinib citrate inhibits IL-2-mediated human T cell blast proliferation and IL-15-induced CD69 expression with IC50 of 11 nM and 48 nM, respectively. Tofacitinib citrate prevents mixed lymphocyte reaction with IC50 of 87 nM. Tofacitinib citrate treatment of murine factor-dependent cell Patersen–erythropoietin receptor (FDCP-EpoR) cells harboring human wild-type or V617F JAK2 leads to prevention of cell proliferation with IC50 of 2.1 µM and 0.25 µM, respectively. Tofacitinib citrate inhibits interleukin-6-induced phosphorylation of STAT1 and STAT3 with IC50 of 23 nM and 77 nM, respectively. Moreover, Tofacitinib citrate generates a significant pro-apoptotic effect on murine FDCP-EpoR cells carrying JAK2VV617F, whereas a lesser effect is observed for cells carrying wild-type JAK2. This activity is coupled with the inhibition of phosphorylation of the key JAK2V617F-dependent downstream signaling effectors signal transducer and activator of transcription (STAT)3, STAT5, and v-akt murine thymoma viral oncogene homolog (AKT). Additionally, Tofacitinib citrate prevents IL-15-induced CD69 expression in human and cynomolgus monkey NK and CD8+ T cells in vitro. |
| In vivo(体内研究) | Tofacitinib citrate decrease a delayed-type hyper-sensitivity response and extended cardiac allograft survival in murine models. Furthermore, Tofacitinib citrate treatment of ex-vivo-expanded erythroid progenitors from JAK2V617F-positive PV patients results in specific, antiproliferative (IC50 = 0.2 μM) and pro-apoptotic activity. In contrast, expanded progenitors from healthy controls are less sensitive to Tofacitinib citrate in proliferation (IC50 > 1.0 μM), and apoptosis assays. During 2 weeks of Tofacitinib citrate dosing at 10 and 30 mg/kg/d, a significant, time-dependent decrease in NK cell numbers relative to vehicle treatment is observed. Effector memory CD8+ cell numbers in the Tofacitinib citrate-treated group are 55% less than those observed in animals treated with vehicle. |
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| 研究领域 | |
| 研究领域 | CancerOncoproteins/suppressorsOncoproteinsSignal transducers CancerSignal transductionProtein phosphorylationTyrosine kinasesOther EpigeneticsNuclear Signaling PathwaysSTATs EpigeneticsTranscriptionTranscription Factors Signal TransductionProtein PhosphorylationTyrosine KinasesOther Signal TransductionSignaling PathwayNuclear SignalingSTATs Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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