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枸橼酸托法替尼 /Tofacitinib citrate {[allProObj[0].p_purity_real_show]}

货号:A118834 同义名: 柠檬酸托法替尼 / Tasocitinib citrate;CP-690550 citrate

Tofacitinib citrate是一种口服有效的JAK1/2/3抑制剂,其IC50值分别为1、20和112 nM。它还具有抗细菌、抗真菌抗病毒特性。

Tofacitinib citrate 化学结构 CAS号:540737-29-9
Tofacitinib citrate 化学结构
CAS号:540737-29-9
Tofacitinib citrate 3D分子结构
CAS号:540737-29-9
Tofacitinib citrate 化学结构 CAS号:540737-29-9
Tofacitinib citrate 3D分子结构 CAS号:540737-29-9
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Tofacitinib citrate 纯度/质量文件 产品仅供科研

货号:A118834 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 JAK1 JAK2 JAK3 Tyk2 其他靶点 纯度
Decernotinib +++

JAK1, Ki: 11 nM

JAK1, IC50: 11 nM

+++

JAK2, Ki: 13 nM

++++

JAK3, Ki: 2.5 nM

+++

TYK2, Ki: 13 nM

99%+
ZM39923 HCl +

JAK1, pIC50: 4.4

+

JAK3, pIC50: 7.1

EGFR 97%
Cerdulatinib +++

JAK1, IC50: 12 nM

+++

JAK2, IC50: 6 nM

+++

JAK3, IC50: 8 nM

++++

TYK2, IC50: 0.5 nM

99%+
Momelotinib +++

JAK1, IC50: 11 nM

++

JAK2, IC50: 18 nM

+

JAK3, IC50: 155 nM

99%+
XL019 +

JAK1, IC50: 134.3 nM

++++

JAK2, IC50: 2.2 nM

+

JAK3, IC50: 214.2 nM

FLT3 99%+
Ruxolitinib +++

JAK1, IC50: 3.3 nM

++++

JAK2, IC50: 2.8 nM

98%
Tofacitinib +

JAK1, IC50: 112 nM

++

JAK2, IC50: 20 nM

++++

JAK3, IC50: 1 nM

98%
Ruxolitinib (S enantiomer) +++

JAK1, IC50: 3.3 nM

++++

JAK2, IC50: 2.8 nM

++

TYK2, IC50: 19 nM

98%
Filgotinib +++

JAK1, IC50: 10 nM

++

JAK2, IC50: 28 nM

+

JAK3, IC50: 810 nM

+

TYK2, IC50: 116 nM

99%
Baricitinib +++

JAK1, IC50: 5.9 nM

+++

JAK2, IC50: 5.7 nM

++

TYK2, IC50: 53 nM

99%
Gandotinib ++

JAK1, IC50: 19.8 nM

++++

JAK2, IC50: 0.288 nM

JAK2 (V617F), Ki: 0.245 nM

++

JAK3, IC50: 48.0 nM

++

TYK2, IC50: 44 nM

FLT3 99%+
Oclacitinib maleate +++

JAK1, IC50: 10nM

++

JAK2, IC50: 18nM

+

JAK3, IC50: 99nM

+

TYK2, IC50: 84nM

98+%
NVP-BSK805 2HCl ++

JAK1, IC50: 31.63 nM

++++

JAK2, IC50: ~0.5 nM

++

JAK3, IC50: 18.68 nM

+++

TYK2, IC50: 10.76 nM

99+%
Peficitinib 98%
Go6976 FLT3 99%+
AZD-1480 ++++

JAK2, IC50: 0.26 nM

99%+
Fedratinib +++

JAK2 (V617F), IC50: 3 nM

JAK2, IC50: 3 nM

FLT3,RET 99%+
WP1066 +

JAK2, IC50: 2.3 μM

98%
Curcumol 98%
AZ960 ++++

JAK2, Ki: 0.45 nM

JAK2, IC50: <3 nM

97%
GLPG0634 analog 99%+
CEP-33779 ++++

JAK2, IC50: 1.8 nM

99%+
FLLL32 +

JAK2, IC50: <5 μM

99%+
WHI-P154 +

JAK3, IC50: 1.8 μM

EGFR,Src,VEGFR 98%
BMS-911543 ++++

JAK2, IC50: 1.1 nM

+

JAK3, IC50: 75 nM

++

TYK2, IC50: 66 nM

98%
TG101209 +++

JAK2, IC50: 6 nM

+

JAK3, IC50: 169 nM

FLT3,RET 99%+
AT9283 ++++

JAK2, IC50: 1.2 nM

++++

JAK3, IC50: 1.1 nM

99%+
Pacritinib ++

JAK2 (V617F), IC50: 19 nM

JAK2, IC50: 23 nM

+

JAK3, IC50: 520 nM

++

TYK2, IC50: 50 nM

FLT3 97%
Tofacitinib citrate ++

JAK2, IC50: 20 nM

++++

JAK3, IC50: 1 nM

99%
FM-381 ++++

JAK3, IC50: 127 pM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Tofacitinib citrate 生物活性

靶点
  • JAK3

    JAK3, IC50:1 nM

  • JAK2

    JAK2, IC50:20 nM

描述 Tofacitinib Citrate is the citrate form of Tofacitinib. Tofacitinib is an ATP-competed inhibitor of JAK with IC50 values of 3.2±1.4 nM, 4.1±0.4 nM, 1.6±0.2 nM, 34.0±6.0 nM for JAK1, JAK2, JAK3 and TYK2 in in vitro enzyme assays. It competes with ATP for binding to the active site of the kinase domain of JAKs with Ki values of 0.68 ± 0.12 nM (JAK1), 0.99 ± 0.04 nM (JAK2), 0.24 ± 0.02 nM (JAK3) and 4.39 ± 0.27 nM (TYK2). Tofacitinib potently inhibits multiple cytokine activated JAK/STAT signaling pathways in normal human, mouse or rat whole blood with IC50s below 200 nM. Selectivity assessed in mouse and rat whole blood shows that tofacitinib appears to be more potently to JAK1 and JAK3. In cell assays, tofacitinib inhibits human total myeloid and CFU-G colony formation with IC50s of 0.87 and 0.93 μM. In AIA rats, tofacitinib treatment can decrease paw volume and disease-elevated neutrophil count to normal range compared to vehicle treated control rats. Tofacitinib treatment also dose-dependently decreased both IL-17 and IL-6 of the AIA-induced increase compared to control levels with an approximately 80% inhibition. It significantly inhibits the AIA-induced increase in maturing myeloid cells by approximately 50% at the 10 mg/kg dose[3]. Tofacitinib has been approved by the U.S. Food and Drug Administration and European Medicines Agency for the treatment of rheumatoid arthritis (RA), psoriatic arthritis and ulcerative colitis[1].

Tofacitinib citrate 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
Ba/F3 cells Function assay 60 mins Inhibition of TEL-fused JAK1 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay, IC50=26 nM. 22087750
Ba/F3 cells Function assay 60 mins Inhibition of TEL-fused JAK3 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay, IC50=54 nM. 22087750
human CD4+ T cells 5 to 500 nM Function assay 1 h Inhibition of IL2-induced Stat5 phosphorylation in human CD4+ T cells at 5 to 500 nM after 1 hr by Western blot 19053756
human DND/L12 cells Function assay 30 mins Inhibition of JAK3 in human DND/L12 cells after 30 mins by luciferase assay in presence of human serum albumin. 14593182

Tofacitinib citrate 动物研究

Dose Rat: 5 mg/kg - 50 mg/kg[3] (i.v.), 10 mg/kg - 100 mg/kg[4] (p.o.) Mice: 1 mg/kg - 100 mg/kg[5] (p.o.)
Administration i.v., p.o.

Tofacitinib citrate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01023100 Arthritis, Rheumatoid Phase 1 Completed - United States, Massachusetts ... 展开 >> Pfizer Investigational Site Woburn, Massachusetts, United States, 01801 收起 <<
NCT01185184 Healthy Phase 1 Completed - Singapore ... 展开 >> Pfizer Investigational Site Singapore, Singapore, 188770 收起 <<
NCT01246583 Psoriasis Phase 2 Completed - United States, Alabama ... 展开 >> Pfizer Investigational Site Mobile, Alabama, United States, 36606 United States, California Pfizer Investigational Site Los Angeles, California, United States, 90045 United States, Florida Pfizer Investigational Site Orange Park, Florida, United States, 32073 United States, Nebraska Pfizer Investigational Site Omaha, Nebraska, United States, 68144 United States, New Mexico Pfizer Investigational Site Albuquerque, New Mexico, United States, 87106 United States, South Dakota Pfizer Investigational Site Rapid City, South Dakota, United States, 57702 United States, Texas Pfizer Investigational Site Dallas, Texas, United States, 75231 Canada, Ontario Pfizer Investigational Site Waterloo, Ontario, Canada, N2J 1C4 Canada, Quebec Pfizer Investigational Site Montreal, Quebec, Canada, H2K 4L5 Pfizer Investigational Site Montreal, Quebec, Canada, H3Z 2S6 Canada Pfizer Investigational Site Quebec, Canada, G1V 4X7 收起 <<

Tofacitinib citrate 参考文献

[1]Meyer DM, Jesson MI, Li X, Elrick MM, Funckes-Shippy CL, Warner JD, Gross CJ, Dowty ME, Ramaiah SK, Hirsch JL, Saabye MJ, Barks JL, Kishore N, Morris DL. Anti-inflammatory activity and neutrophil reductions mediated by the JAK1/JAK3 inhibitor, CP-690,550, in rat adjuvant-induced arthritis. J Inflamm (Lond). 2010 Aug 11;7:41. doi: 10.1186/1476-9255-7-41. PMID: 20701804; PMCID: PMC2928212.

[2]Lloyd-Lavery A. Long-term safety data for tofacitinib, an oral Janus kinase inhibitor, for the treatment for psoriasis. Br J Dermatol. 2018;179(4):815-816.

[3]Lloyd-Lavery A. Long-term safety data for tofacitinib, an oral Janus kinase inhibitor, for the treatment for psoriasis. Br J Dermatol. 2018 Oct;179(4):815-816. doi: 10.1111/bjd.17016. PMID: 30318813.

Tofacitinib citrate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.91mL

1.98mL

0.99mL

19.82mL

3.96mL

1.98mL

Tofacitinib citrate 技术信息

CAS号540737-29-9
分子式C22H28N6O8
分子量 504.493
别名 柠檬酸托法替尼 ;Tasocitinib citrate;CP-690550 citrate;CP 690,550;Tofacitinib (citrate)
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 25 mg/mL(49.55 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 3 mg/mL(5.95 mM),配合低频超声助溶

动物实验配方

IP 2% DMSO+water 2 mg/mL clear

PO 0.5% CMC-Na 80 mg/mL suspension

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