首页工具

购物车

Ritlecitinib

产品编号 T5382 CAS 1792180-81-4

别名: PF-06651600

Ritlecitinib (PF-06651600) 是一种口服有效的选择性JAK3抑制剂，IC50值为 33.1 nM。

TargetMol的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

Ritlecitinib, CAS 1792180-81-4

规格	价格/CNY	货期
2 mg	￥ 297	现货
5 mg	￥ 483	现货
10 mg	￥ 778	现货
25 mg	￥ 1,560	现货
50 mg	￥ 2,480	现货
100 mg	￥ 3,690	现货
200 mg	￥ 5,230	现货
500 mg	￥ 7,930	现货
1 mL * 10 mM (in DMSO)	￥ 535	现货

大包装超大折扣，点击咨询

其他形式的 Ritlecitinib:

选择批次

纯度: 99.92%

纯度: 99.1%

纯度: 98.92%

纯度: 98.82%

纯度: 98.81%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Ritlecitinib (PF-06651600) is a potent JAK3-selective inhibitor (IC50: 33.1 nM).
靶点活性	JAK3:33.1 nM (cell free)
体外活性	PF-06651600 inhibited JAK3 kinase activity with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2. In total lymphocytes in human whole blood, PF-06651600 inhibited the phosphorylation of STAT5 elicited by IL-2, IL-4, IL-7, and IL-15 with IC50 values of 244, 340, 407, and 266 nM, respectively, and it inhibited the phosphorylation of STAT3 elicited by IL-21 with an IC50 of 355 nM [1].
体内活性	In the rat adjuvant-induced arthritis (AIA) model, PF-06651600 reduced paw swelling with an unbound EC50 of 169 nM. Similarly, PF-06651600 significantly reduced disease severity in the experimental autoimmune encephalomyelitis21,22 (EAE) mouse model when dosed either therapeutically at 30 or 100 mg/kg or prophylactically at 20 and 60 mg/kg [1].
激酶实验	His-tagged recombinant human TYK2 kinase domain was expressed in SF21/baculovirus and purified using a two-step affinity (Ni-NTA) and size-exclusion (SEC S200) purification method.Test compounds were solubilized in DMSO to a stock concentration of 30 mM.Compounds were diluted in DMSO to create an 11-point half log dilution series with a top concentration of 600 μM.The test compound plate also contained positive control wells containing a known inhibitor to define 100% inhibition and negative control wells containing DMSO to define no inhibition.The compound plates were diluted 1 to 60 in the assay,resulting in a final assay compound concentration range of 10 μM to 100 pM and a final assay concentration of 1.7% DMSO.Test compounds and controls solubilized in 100% DMSO were added (250 nL) to a 384 well polypropylene plate (Matrical) using a non contact acoustic dispenser.Kinase assays were carried out at room temperature in a 15 μL reaction buffer containing 20 mM HEPES,pH 7.4,10 mM magnesium chloride,0.01% bovine serum albumin (BSA),0.0005% Tween 20 and 1mM Dithiothreitol (DTT).Reaction mixtures contained 1 μM of a fluorescently labeled synthetic peptide,at a concentration less than the apparent Michaelis-Menten constant (Km) (5FAM-KKSRGDYMTMQID for JAK1 and TYK2 and FITC-KGGEEEEYFELVKK for JAK2 and JAK3).Reaction mixtures contained adenosine triphosphate (ATP) at either a level equal to the apparent Km for ATP (40 μM for JAK1,4 μM for JAK2,4 μM for JAK3 and 12 μM for TYK2) or at 1 mM ATP.Compound was added to the buffer containing ATP and substrate and immediately after this step the enzyme was added to begin the reaction.The assays were stopped with 15 μL of a buffer containing 180 mM HEPES,pH=7.4,20 mM EDTA,0.2% Coating Reagent,resulting in a final concentration of 10 mM EDTA,0.1% Coating Reagent and 100 mM HEPES,pH=7.4.
细胞实验	Human CD4+ T cells were purified from buffy coat with RosetteSep CD4+ T Cell Enrichment Cocktail and skewed for 6 days with cytokine cocktails (25 ng/mL of IL-6, 25 ng/mL of IL-23, 12.5 ng/mL of IL-1β, 25 ng/mL of IL21, 5 ng/mL of TGFβ1, 10 μg/ml of anti-CD3 antibody (pre-coated on plate surface) and 1 μg/mL of anti-CD28 antibody) in the presence of JAK inhibitors at 10 different concentrations. Supernatants were harvested and the concentrations of IL-17A were determined with MSD assay following the protocol provided by the manufacturer. To study the effect of PF-06651600 on Th17 cells post-differentiation, skewed Th17 cells were washed, rested with X-VIVO 15 medium for overnight and resuspended in medium containing the same concentrations of cytokines as during skewing but without anti-CD3 or anti-CD28 antibodies, in the presence of PF-06651600 at 10 different concentrations for 2 additional days. On Day 9, supernatant was harvested from each well and IL-17A was determined as described above [1].
动物实验	The effect of JAK3 inhibition by PF-06651600 was evaluated in vivo using a therapeutic dosing paradigm in a rat adjuvant-induced arthritis. The efficacy of this molecule was evaluated in three separate studies using successively lower doses. Arthritis was induced by immunization of female Lewis rats (8 to 10 weeks old) via intradermal injection at the base of the tail with complete Freund's adjuvant with three 50 μL injections (15 mg/mL Mycobacterium tuberculosis) in incomplete Freund's adjuvant. Seven days after the initial immunization, the baseline hind paw volume of the immunized rats was measured via plethysmograph. The rats were monitored daily for signs of arthritis including change in body weight and hind paw volume measurement. When individual hind paw volume measurements indicated an increase of 0.2 mL (or greater) in a single hind paw, animals were randomly assigned to a treatment group. Daily treatment with PF-06651600 was administered via oral gavage. Treatment groups for Experiment 1 were: 80, 15, or 6 mg/kg or vehicle (2% Tween 80 /0.5% methylcellulose/deionized water). Treatment groups for Experiment 2 were: 30, 10, and 3 mg/kg or vehicle (0.5% methylcellulose / de-ionized water/ 1 mEQ hydrochloric acid). Treatment groups for Experiment 3 were: 10, 1, 0.3 and 0.1 mg/kg or vehicle (0.5% methylcellulose/de-ionized water/ 1 mEQ hydrochloric acid). Dosing began once individuals were enrolled into respective groups. Treatment continued for 7 days. At the conclusion of the study, whole blood was taken at 15 minutes post-dose (peak concentration in plasma) for analysis of STAT phosphorylation, and plasma was taken for exposure concentration in PF-06651600 dosed groups [1].

别名	PF-06651600
分子量	285.34
分子式	C15H19N5O
CAS No.	1792180-81-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 130 mg/mL (455.60 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.5046 mL	17.523 mL	35.0459 mL	87.6148 mL
	5 mM	0.7009 mL	3.5046 mL	7.0092 mL	17.523 mL
	10 mM	0.3505 mL	1.7523 mL	3.5046 mL	8.7615 mL
	20 mM	0.1752 mL	0.8761 mL	1.7523 mL	4.3807 mL
	50 mM	0.0701 mL	0.3505 mL	0.7009 mL	1.7523 mL
	100 mM	0.035 mL	0.1752 mL	0.3505 mL	0.8761 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Telliez JB, et al. Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition. ACS Chem Biol. 2016 Dec 16;11(12):3442-3451. 2. Thorarensen A, et al. Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans. J Med Chem. 2017 Mar 9;60(5):1971-1993.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

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。

Keywords

Ritlecitinib 1792180-81-4 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells JAK Janus kinase Inhibitor inhibit PF06651600 PF-06651600 PF 06651600 inhibitor

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

沪公网安备 31010602006700号

陶术

生物

TargetMol^®中国区唯一合作伙伴

点击进入陶术生物官网

联系我们

电话：

400-820-0310

邮箱：

service@tsbiochem.com

QQ：

2881945090（终端用户）

2885109491（经销商）

经销：

终端：

地址：

上海市静安区江场三路238号8楼

Ritlecitinib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords