Oclacitinib maleate | PF-03394197 maleate;PF-03394197;Oclacitinib maleate | JAK

首页 / / / JAK / Oclacitinib maleate

奥拉替尼马来酸盐 /Oclacitinib maleate {[allProObj[0].p_purity_real_show]}

货号：A265661 同义名： PF-03394197 maleate;PF-03394197

Oclacitinib Fumarate is a potent JAK inhibitor with IC50 value ranging in 10-99 nM for JAK family members, most potent against JAK1 with IC50 value of 10 nM.

Oclacitinib maleate 化学结构
CAS号：1640292-55-2

Oclacitinib maleate 3D分子结构
CAS号：1640292-55-2

规格	价格	会员价	库存	数量
{[ item.pr_size ]}	{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]}	{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]}	{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_am, item.pr_size) ]}	{[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]}	现货	咨询	- +

购物车0 收藏询单

sales@ambeed.cn tech@ambeed.cn 400-920-2911 产品手册产品订购技术咨询
快速发货顺丰冷链运输，1-2 天到达

品质保证

技术支持

免费溶解

Oclacitinib maleate 纯度/质量文件产品仅供科研

货号：A265661 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: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 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		99+%
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		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, 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。

Oclacitinib maleate 生物活性

靶点

JAK1

JAK1, IC50:10nM
JAK3

JAK3, IC50:99nM
Tyk2

TYK2, IC50:84nM
JAK2

JAK2, IC50:18nM

描述

Janus kinase (JAK) enzymes are a family of tyrosine kinases consisting of four members: JAK1, JAK2, JAK3, and TYK2. Oclacitinib is a potent JAK1 inhibitor with an IC50 value of 10nM. It also inhibits JAK2, JAK3, and TYK2 with IC50 values of 18, 99, and 84nM, respectively. Oclacitinib inhibited the function of JAK1-dependent cytokines involved in allergy, inflammation, and pruritus, including interleukin (IL)-2, IL-4, IL-6, IL-13, and IL-31 with IC50 values ranging from 36 to 249nM^[3]. In a mouse model of toluene-2,4-diisocyanate (TDI)-induced allergic dermatitis, topical administration of Oclacitinib (0.1%, 0.25%, and 0.5%) 30 minutes before and 4 h after TDI challenge resulted in a significant decrease in scratching behavior and ear thickness, as well as a reduction in the levels of inflammatory cytokines in the ear skin compared with the vehicle-treated group^[4].

Oclacitinib maleate 参考文献

[1]Gonzales AJ, Bowman JW, et al. Oclacitinib(APOQUEL(®)) is a novel Janus kinase inhibitor with activity against cytokines involved in allergy. J Vet Pharmacol Ther. 2014 Aug;37(4):317-24.

[2]Collard WT, Hummel BD, et al. The pharmacokinetics of oclacitinib maleate, a Janus kinase inhibitor, in the dog. J Vet Pharmacol Ther. 2014 Jun;37(3):279-85.

[3]Gonzales AJ, Bowman JW, Fici GJ, Zhang M, Mann DW, Mitton-Fry M. Oclacitinib (APOQUEL(®)) is a novel Janus kinase inhibitor with activity against cytokines involved in allergy. J Vet Pharmacol Ther. 2014;37(4):317-324. doi:10.1111/jvp.12101

[4]Fukuyama T, Ehling S, Cook E, Bäumer W. Topically Administered Janus-Kinase Inhibitors Tofacitinib and Oclacitinib Display Impressive Antipruritic and Anti-Inflammatory Responses in a Model of Allergic Dermatitis. J Pharmacol Exp Ther. 2015;354(3):394-405. doi:10.1124/jpet.115.223784

Oclacitinib maleate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.03mL

2.21mL

1.10mL

22.05mL

4.41mL

2.21mL

Oclacitinib maleate 技术信息

CAS号	1640292-55-2
分子式	C₁₉H₂₇N₅O₆S
分子量	453.51

别名	PF-03394197 maleate;PF-03394197;Oclacitinib maleate
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

DMSO: 250 mg/mL(551.25 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: 5 mg/mL(11.03 mM)，配合低频超声助溶

动物实验配方

PO 0.5% CMC-Na 30 mg/mL suspension

奥拉替尼马来酸盐 /Oclacitinib maleate {[allProObj[0].p_purity_real_show]}

Oclacitinib maleate 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Oclacitinib maleate 质控信息

Oclacitinib maleate 生物活性

Oclacitinib maleate 参考文献

Oclacitinib maleate 实验方案

Oclacitinib maleate 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

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

JAK1	JAK1, IC50:10nM
JAK3	JAK3, IC50:99nM
Tyk2	TYK2, IC50:84nM
JAK2	JAK2, IC50:18nM

奥拉替尼马来酸盐 /Oclacitinib maleate {[allProObj[0].p_purity_real_show]}

Oclacitinib maleate 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Oclacitinib maleate 质控信息

Oclacitinib maleate 生物活性

Oclacitinib maleate 参考文献

Oclacitinib maleate 实验方案

Oclacitinib maleate 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

请登录您的专属账户

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

Oclacitinib maleate 纯度/质量文件产品仅供科研