Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tofacitinib Citrate (CP-690550 citrate) 是 JAK1/2/3抑制剂,IC50分别为112,20 和 1 nM。它具有抗菌,抗真菌和抗病毒活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 297 | 现货 | ||
10 mg | ¥ 497 | 现货 | ||
25 mg | ¥ 828 | 现货 | ||
50 mg | ¥ 1,230 | 现货 | ||
100 mg | ¥ 1,980 | 现货 | ||
200 mg | ¥ 3,510 | 现货 | ||
500 mg | ¥ 5,350 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 547 | 现货 |
产品描述 | Tofacitinib Citrate (CP-690550 citrate) is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM). |
靶点活性 | JAK2:20 nM (cell free), JAK1:112 nM (cell free), JAK3:1 nM (cell free) |
体外活性 | Although Tofacitinib (CP-690,550) was highly potent for JAK3 inhibition (enzyme inhibitory potency of 1 nM), it was 20- to 100-fold less potent for JAK2 and JAK1, respectively. CP-690,550 inhibited IL-2-induced proliferation with 30-fold greater potency than its effects on GM-CSF-induced proliferation. CP-690,550 demonstrated potent inhibition in the mixed lymphocyte reaction using murine, monkey, or human cells. Consistent with its mechanism of action, these cellular activities correlated with the ability of CP-690,550 to block IL-2-induced phosphorylation of JAK3 and one of its key substrates, STAT5 [1]. CP-690,550 treatment of murine factor-dependent cell Patersen-erythropoietin receptor (FDCP-EpoR) cells harboring human wild-type or V617F JAK2 resulted in inhibition of cell proliferation with an IC50 of 2.1 microM and 0.25 microM, respectively. CP-690,550 treatment of ex-vivo-expanded erythroid progenitors from JAK2(V617F)-positive PV patients resulted in specific, antiproliferative (IC50: 0.2 microM) and pro-apoptotic activity [2]. The pharmacological inhibition of JAK3 by tofacitinib synergistically enhanced the antitumor effects of IMA in CML cells [3]. |
体内活性 | CP-690,550 treatment significantly prolonged graft survival as compared to vehicle. Four of 12 animals dosed with CP-690,550 (two from each dose group) survived to study termination with normal renal function and mild rejection as determined by histopathology [1]. Monotherapy of mice with tofacitinib quells Ab responses to an immunotoxin derived from the bacterial protein Pseudomonas exotoxin A, as well as to the model Ag keyhole limpet hemocyanin. Thousand-fold reductions in IgG1 titers to both Ags were observed 21 d post immunization. Tofacitinib treatment led to reduced numbers of CD127+ pro-B cells [4]. |
激酶实验 | The JAK1, JAK2, and JAK3 kinase assays utilize a protein expressed in baculovirus-infected SF9 cells (a fusion protein of GST and the catalytic domain of human JAK enzyme) purified by affinity chromatography on glutathione sepharose. The substrate for the reaction was polyglutamic acid-tyrosine [PGT (4:1)], coated onto Nunc Maxi Sorp plates at 100 μg/mL overnight at 37 °C. The plates were washed three times, and JAK enzyme was added to the wells, which contained 100 μL of kinase buffer (50 mM HEPES, pH 7.3, 125 mM NaCl, 24 mM MgCl2) + ATP + 1 mM sodium orthovanadate). After incubation at room temperature for 30 min, the plates were washed three times. The level of phosphorylated tyrosine in a given well was determined by standard ELISA assay utilizing an anti-phosphotyrosine antibody [5]. |
细胞实验 | Apoptotic cells were detected by flow cytometry using recombinant human Annexin-V conjugated with allophycocyanin. Briefly, after exposure to CP-690,550 for different periods of time, cells were washed in Ca2+-free PBS and resuspended in 100 μL of binding buffer (10 mM HEPES pH 7.4; 0.15 M NaC1; 5 mM KCl; 1 mM MgCl2; 1.8 mM CaCl2) to which Annexin-V-APC had been previously added. Cells were incubated for 20 min in the dark at room temperature, washed and resuspended in 0.3 mL binding buffer. Cells were analyzed on a FACSCalibur flow cytometer equipped with the Cell Quest Pro software [2]. |
动物实验 | Mice received tofacitinib in PEG300 (100 mg/ml) or vehicle alone (PEG300) by osmotic pump infusion (Alzet Model 2004, 0.25 μl/hour, 28 days). Four days prior to immunization, mice were anesthetized and their dorsal surface was shaved. A one cm incision was made on the back to create a subcutaneous pocket and insert the pump. The incision site was closed with wound clips. Mice were injected weekly (i.p.) with SS1P recombinant immunotoxin (RIT; 5 μg/mouse) beginning on day 0; control mice received injections of saline alone. Every week before SS1P or vehicle immunization, ~50 μl of blood was drawn to obtain serum samples. Sera were stored at ?80°C until analyzed [4]. |
别名 | CP-690550 citrate, 柠檬酸托法替尼, 枸橼酸托法替尼, Tasocitinib citrate, Tofacitinib (CP-690550) Citrate |
分子量 | 504.49 |
分子式 | C22H28N6O8 |
CAS No. | 540737-29-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50.5 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9822 mL | 9.911 mL | 19.822 mL | 49.555 mL |
5 mM | 0.3964 mL | 1.9822 mL | 3.9644 mL | 9.911 mL | |
10 mM | 0.1982 mL | 0.9911 mL | 1.9822 mL | 4.9555 mL | |
20 mM | 0.0991 mL | 0.4955 mL | 0.9911 mL | 2.4777 mL | |
50 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9911 mL | |
100 mM | 0.0198 mL | 0.0991 mL | 0.1982 mL | 0.4955 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Tofacitinib Citrate 540737-29-9 Angiogenesis Apoptosis Chromatin/Epigenetic JAK/STAT signaling Microbiology/Virology Stem Cells Influenza Virus JAK Antibacterial Antifungal inhibit CP-690550 Citrate CP-690550 citrate 柠檬酸托法替尼 CP-690550 CP690550 Citrate 枸橼酸托法替尼 CP690550 Janus kinase CP 690550 Tasocitinib citrate Fungal CP 690550 Citrate Tasocitinib Citrate Tofacitinib Tofacitinib (CP-690550) Citrate Inhibitor Tasocitinib Bacterial inhibitor