Tofacitinib | Tasocitinib;CP-690550 | JAK | AmBeed-信号通路专用抑制剂

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Tofacitinib/托法替尼 {[allProObj[0].p_purity_real_show]}

货号：A280750 同义名： Tasocitinib; CP-690550

Tofacitinib是一种口服可用的 JAK3/2/1 抑制剂，其 IC50 值分别为 1 nM、20 nM 和 112 nM。

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Tofacitinib/托法替尼化学结构
CAS号：477600-75-2

Tofacitinib/托法替尼 3D分子结构
CAS号：477600-75-2

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Tofacitinib/托法替尼纯度/质量文件产品仅供科研

货号：A280750 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nature, 2025. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Mater., 2025, 24, 1116-1125. Ambeed. [ A141030 , A131652 ]; 更多 >

JAK 亚型比较

产品名称	JAK1 ↓ ↑	JAK2 ↓ ↑	JAK3 ↓ ↑	Tyk2 ↓ ↑	其他靶点	纯度
Decernotinib	+++ JAK1, IC50: 11 nM JAK1, Ki: 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		95%
Peficitinib		✔				98%
Go6976		✔			FLT3	99%+
AZD-1480		++++ JAK2, IC50: 0.26 nM				99%+
Fedratinib		+++ JAK2, IC50: 3 nM JAK2 (V617F), IC50: 3 nM			FLT3,RET	99%+
WP1066		+ JAK2, IC50: 2.3 μM				98%
Curcumol		✔				98%
AZ960		++++ JAK2, IC50: <3 nM JAK2, Ki: 0.45 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		Src,EGFR,VEGFR	98%
BMS-911543		++++ JAK2, IC50: 1.1 nM	+ JAK3, IC50: 75 nM	++ TYK2, IC50: 66 nM		95%
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, IC50: 23 nM JAK2 (V617F), IC50: 19 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/托法替尼生物活性

靶点

JAK1

JAK1, IC50:112 nM
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^[6]. 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^[2].

Tofacitinib/托法替尼细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	数据源
CD4+ T	20/100/500 nM	Function Assay	48 h	inhibits the levels of IL-4, IFN-γ, IL-17A and IL-22	21884580
CD4+ T	100/500 nM	Growth Inhibition Assay	48 h	inhibits anti-CD3-induced CD4+ T cell proliferation	21884580
CD4+ T	100 nM	Function Assay	24/48 h	abrogates CD3-induced phosphorylation of STATs	21884580
T cells	0.1/0.3/1 μM	Function Assay	24 h	disrupts γc-chain cytokine signaling	21383241

Tofacitinib/托法替尼动物研究

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.

Pharmacokinetics

Animal	Rats^[4]	Dogs^[4]	Monkeys^[4]
Dose	3 mg/kg or 10 mg/kg (i.v.) 10 mg/kg (p.o., water)	3 mg/kg (i.v.) 5 mg/kg (p.o., 0.5% methylcellulose)	3 mg/kg (i.v.) 5 mg/kg (p.o., 0.5% methylcellulose)
Administration	i.v. p.o.	i.v. p.o.	i.v. p.o.
F	43.3% (p.o.)	43.0% (p.o.)	48.0% (p.o.)
T_1/2	0.6 ± 0.1 h (i.v.) 2.0 ± 1.5 h (p.o.)	1.2 ± 0.1 h (i.v.)	2.1 ± 0.4 h (i.v.)
T_max	0.3 ± 0.1 h (p.o.)	0.5 ± 0.4 h (p.o.)	1.1 ± 0.9 h (p.o.)
CL	62 ± 14 ml/min/kg (i.v.)	19 ± 10 ml/min/kg (i.v.)	18 ± 4 ml/min/kg (i.v.)
C_max	2400 ± 948 ng/ml (p.o.)	1020 ± 255 ng/ml (p.o.)	791 ± 157 ng/ml (p.o.)
AUC_0→∞	840 ± 184 ng·h/ml (i.v.) 2770 ± 837 ng·h/ml (p.o.)	3250 ± 1610 ng·h/ml (i.v.) 2330 ± 423 ng·h/ml (p.o.)	2850 ± 543 ng·h/ml (i.v.) 2280 ± 338 ng·h/ml (p.o.)
Vss	2.6 ± 1.3 L/kg (i.v.)	1.8 ± 0.8 L/kg (i.v.)	1.7 ± 0.2 L/kg (i.v.)

Tofacitinib/托法替尼参考文献

[1]Meyer DM, Jesson MI, et al. 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.

[2]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.

[3]Lee JS, Kim SH, et al. Dose-Dependent Pharmacokinetics of Tofacitinib in Rats: Influence of Hepatic and Intestinal First-Pass Metabolism. Pharmaceutics. 2019 Jul 5;11(7). pii: E318.

[4]Tofacitinib

[5]Xeljanz

[6]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/托法替尼实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.20mL

0.64mL

0.32mL

16.01mL

3.20mL

1.60mL

32.01mL

6.40mL

3.20mL

Tofacitinib/托法替尼技术信息

CAS号	477600-75-2
分子式	C₁₆H₂₀N₆O
分子量	312.37
SMILES Code	N#CCC(N1C[C@H](N(C)C2=C3C(NC=C3)=NC=N2)[C@H](C)CC1)=O
MDL No.	MFCD11035919

别名	Tasocitinib; CP-690550
运输	蓝冰
InChI Key	UJLAWZDWDVHWOW-YPMHNXCESA-N
Pubchem ID	9926791

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 120 mg/mL(384.16 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

无水乙醇: 2.5 mg/mL(8 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

方案三

方案四

配制的工作液建议现用现配，短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

Tofacitinib/托法替尼 {[allProObj[0].p_purity_real_show]}

Tofacitinib/托法替尼纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Tofacitinib/托法替尼质控信息

Tofacitinib/托法替尼生物活性

Tofacitinib/托法替尼细胞研究

Tofacitinib/托法替尼动物研究

Tofacitinib/托法替尼参考文献

Tofacitinib/托法替尼实验方案

Tofacitinib/托法替尼技术信息

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摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

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JAK1	JAK1, IC50:112 nM
JAK3	JAK3, IC50:1 nM
JAK2	JAK2, IC50:20 nM

Tofacitinib/托法替尼 {[allProObj[0].p_purity_real_show]}

Tofacitinib/托法替尼 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Tofacitinib/托法替尼 质控信息

Tofacitinib/托法替尼 生物活性

Tofacitinib/托法替尼 细胞研究

Tofacitinib/托法替尼 动物研究

Tofacitinib/托法替尼 参考文献

Tofacitinib/托法替尼 实验方案

Tofacitinib/托法替尼 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Tofacitinib/托法替尼纯度/质量文件产品仅供科研

Tofacitinib/托法替尼质控信息

Tofacitinib/托法替尼生物活性

Tofacitinib/托法替尼细胞研究

Tofacitinib/托法替尼动物研究

Tofacitinib/托法替尼参考文献

Tofacitinib/托法替尼实验方案

Tofacitinib/托法替尼技术信息