1. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt
  2. JAK
  3. Decernotinib

Decernotinib  (Synonyms: VX-509; VRT-831509)

目录号: HY-12469 纯度: 99.67%
COA 产品使用指南

Decernotinib 是一种有效的,可口服的 JAK3 抑制剂,对 JAK3JAK1,JAK2 和 TYK2Ki 值分别为 2.5,11,13 和 11 nM。

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Decernotinib Chemical Structure

Decernotinib Chemical Structure

CAS No. : 944842-54-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥935
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5 mg ¥850
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10 mg ¥1300
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25 mg ¥2650
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50 mg ¥4000
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100 mg ¥6000
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500 mg   询价  

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查看 JAK 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Decernotinib is a potent, orally active JAK3 inhibitor, with Kis of 2.5, 11, 13 and 11 nM for JAK3, JAK1, JAK2, and TYK2, respectively.

IC50 & Target[1]

JAK3

2.5 nM (Ki)

JAK1

11 nM (Ki)

Tyk2

11 nM (Ki)

JAK2

13 nM (Ki)

FLT3

1 μM (Ki)

ROCK I

1.5 μM (Ki)

GSK3β

1.8 μM (Ki)

CDK2/CycA

2.6 μM (Ki)

PknB

8 μM (IC50)

体外研究
(In Vitro)

Decernotinib (VX-509) 是一种有效的 JAK3 抑制剂,对 JAK3、JAK1、JAK2 和 TYK2 的 Ki 分别为 2.5、11、13 和 11 nM。Decernotinib 有效阻断 T 细胞增殖,平均 IC50 为 170 ± 101 nM,并抑制 IL-2 刺激的 T 细胞增殖 (IC50、140 和 400 nM)。VX-509 对响应 CD40L 和 IL-4 的 B 细胞也具有细胞毒性 (IC50,50 nM)[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Decernotinib (VX-509,10,25,or 50 mg/kg,po) 显著且剂量依赖性地抑制大鼠因注射胶原蛋白而出现的脚踝直径和爪子重量的增加。Decernotinib 可有效减轻大鼠的软骨损伤和骨吸收。Decernotinib (10、25 或 50 mg/kg,po,bid) 抑制迟发型超敏反应小鼠模型中的耳水肿[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

392.38

Formula

C18H19F3N6O

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 50 mg/mL (127.43 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5485 mL 12.7427 mL 25.4855 mL
5 mM 0.5097 mL 2.5485 mL 5.0971 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制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

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.37 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.37 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.67%

参考文献
Kinase Assay
[1]

The effect of Decernotinib on JAK3 activity is assessed by measuring the residual kinase activity of the recombinantly expressed JAK3 kinase domain using a radiometric assay. The final concentrations of the components in the assay are as follows: 100 mM HEPES (pH 7.5), 10 mM MgCl2, 1 mM dithiothreitol (DTT), 0.01% BSA, 0.25 nM JAK3, 0.25 mg/mL polyE4Y, and 5 μM 33P-γ-ATP (200 µCi/µmol). A 10 mM stock solution of Decernotinib is prepared in DMSO, from which additional dilutions are prepared. A substrate mixture (100 mM HEPES, 10 mM MgCl2, 0.5 mg/mL polyE4Y, and 10 μM 33P-γ-ATP) is added and mixed with Decernotinib stock solution. The reaction is initiated by the addition of an enzyme mixture [100 mM HEPES (pH 7.5), 10 mM MgCl2, 2 mM DTT, 0.02% BSA, 0.5 nM JAK3]. After 15 minutes, the reaction is quenched with 20% trichloroacetic acid (TCA). The quenched reaction is transferred to the GF/B filter plates and washed three times with 5% TCA. Following the addition of Ultimate Gold scintillant (50 μL), the samples are counted in a Packard TopCount gamma counter. In this procedure, the radioactivity trapped is a measure of the residual JAK3 kinase activity. From the activity versus concentration of Decernotinib titration curve, the Ki value is determined by fitting the data to an equation for competitive tight binding inhibition kinetics[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Whole-blood samples from healthy volunteers are used to collect peripheral blood mononuclear cells, which are plated in T75 tissue culture flasks at a density of 1 × 106/mL. Cells are stimulated with 10 μg/mL phytohemagglutinin at 37°C for 72 hours. After 72 hours, cells are detached from the flask by scraping, washed, and plated at a density of 1 × 105/well in a 96-well plate. Decernotinib (9.7 nM to 10 μM) is added, and plates are incubated for 30 minutes at 37°C, followed by stimulation with human IL-2. In two rows, only DMSO is added; one row is not stimulated with IL-2, and one row is stimulated with IL-2 to serve as the proliferation control. Plates are incubated at 37°C for 2 days. On day 2, cells are pulsed with 20 µCi/mL methyl-[3H]thymidine for 18-24 hours and harvested onto filters for radiographic determination. Data are analyzed to generate an IC50 value using Softmax pro software[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Rat[1]
The collagen-induced arthritis (CIA) rat model is used to evaluate the effects of oral Decernotinib [10 mg/kg b.i.d., 25 mg/kg b.i.d., 50 mg/kg b.i.d., 50 mg/kg q.d., or 100 mg/kg q.d.] on joint inflammation and histopathology. Female Lewis rats (157-187 g) are anesthetized with isoflurane and injected with 300 µL Freund’s incomplete adjuvant, containing 2 mg/mL bovine type II collagen, at the base of the tail and two sites on the back on days 0 and 6. The rats are randomized to study groups at the onset of paw swelling (arthritis), which occurs between days 10 and 11. Dosing of either Decernotinib or vehicle via oral gavage is initiated on the first day of established arthritis and continued to day 6 of arthritis. Dosing volume is 5 mL/kg. Groups are controls (no collagen injection plus vehicle; n = 4), collagen plus vehicle (n = 5), collagen plus Decernotinib 10 mg/kg b.i.d. (n = 8); collagen plus Decernotinib 10 mg/kg b.i.d. (n = 8); collagen plus (n = 8); collagen plus (n = 8); collagen plus (n = 8); collagen plu (n = 8); and collagen plus (n = 8); collagen plu (n = 8); all treatments are administered for 6 days. An additional group of rats is given collagen plus 10 mg/kg subcutaneous etanercept, a human tumor necrosis factor-α antagonist, on study days 11 and 14. Caliper measurements of normal (baseline) ankle joints begin on day 9 and continue through the last day of study. Differences in mean ankle diameter are tested for significance using Student’s t test, with significance set at P ≤ 0.05. The rats are euthanized on day 7 of arthritis, which is study day 17 or 18 depending on when animals are randomized to groups; paws and knees are harvested to determine paw weight and to conduct a histopathological analysis of inflammation (knee and ankle), pannus formation (ankle), cartilage destruction (knee), and bone resorption (knee and ankle). Scores range from 0 (normal) to 5 (severe pathology) and are assigned by a veterinary pathologist. Percent inhibition is calculated using the following formula: [(mean of treatment group) − (mean of control)] ÷ [(mean of collagen + vehicle) − (mean of control)]. Kruskal-Wallis one-way analysis of variance nonparametric tests are used to determine statistical significance among the histopathology groups, with significance set at P ≤ 0.05[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5485 mL 12.7427 mL 25.4855 mL 63.7137 mL
5 mM 0.5097 mL 2.5485 mL 5.0971 mL 12.7427 mL
10 mM 0.2549 mL 1.2743 mL 2.5485 mL 6.3714 mL
15 mM 0.1699 mL 0.8495 mL 1.6990 mL 4.2476 mL
20 mM 0.1274 mL 0.6371 mL 1.2743 mL 3.1857 mL
25 mM 0.1019 mL 0.5097 mL 1.0194 mL 2.5485 mL
30 mM 0.0850 mL 0.4248 mL 0.8495 mL 2.1238 mL
40 mM 0.0637 mL 0.3186 mL 0.6371 mL 1.5928 mL
50 mM 0.0510 mL 0.2549 mL 0.5097 mL 1.2743 mL
60 mM 0.0425 mL 0.2124 mL 0.4248 mL 1.0619 mL
80 mM 0.0319 mL 0.1593 mL 0.3186 mL 0.7964 mL
100 mM 0.0255 mL 0.1274 mL 0.2549 mL 0.6371 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Decernotinib
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HY-12469
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