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

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托法替尼 /Tofacitinib 98%

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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Type	HazMat fee for 500 gram (Estimated)
Excepted Quantity	USD 0.00
Limited Quantity	USD 15-60
Inaccessible (Haz class 6.1), Domestic	USD 80+
Inaccessible (Haz class 6.1), International	USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic	USD 100+
Accessible (Haz class 3, 4, 5 or 8), International	USD 200+

Tofacitinib 化学结构
CAS号：477600-75-2

Tofacitinib 3D分子结构
CAS号：477600-75-2

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Tofacitinib 纯度/质量文件产品仅供科研

货号：A280750 标准纯度： 98% 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: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

JAK 亚型比较

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, IC50: 3 nM JAK2 (V617F), IC50: 3 nM			RET,FLT3	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		VEGFR,EGFR,Src	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		RET,FLT3	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 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 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	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 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 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 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 技术信息

CAS号	477600-75-2
分子式	C₁₆H₂₀N₆O
分子量	312.37

别名	Tasocitinib;CP-690550
运输	蓝冰

存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

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

动物实验配方

IP 2% DMSO+water 2 mg/mL clear

PO 0.5% CMC-Na 61 mg/mL suspension

托法替尼 /Tofacitinib 98%

Tofacitinib 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 质控信息

Tofacitinib 生物活性

Tofacitinib 细胞研究

Tofacitinib 动物研究

Tofacitinib 参考文献

Tofacitinib 实验方案

Tofacitinib 技术信息

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

托法替尼 /Tofacitinib 98%

Tofacitinib 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 质控信息

Tofacitinib 生物活性

Tofacitinib 细胞研究

Tofacitinib 动物研究

Tofacitinib 参考文献

Tofacitinib 实验方案

Tofacitinib 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 纯度/质量文件产品仅供科研