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  2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt
  3. JAK
  4. Delgocitinib

Delgocitinib  (Synonyms: 迪高替尼; JTE-052)

目錄號(hào): HY-109053 純度: 99.87%
COA 產(chǎn)品使用指南 技術(shù)支持

Delgocitinib (JTE-052) 是一種特異性的 JAK 抑制劑，對(duì) JAK1, JAK2, JAK3 和 Tyk2 的 IC50 值分別為 2.8，2.6，13 和 58 nM。

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Delgocitinib Chemical Structure

Delgocitinib Chemical Structure

CAS No. : 1263774-59-9

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥3850
In-stock
1 mg ￥1580
In-stock
5 mg ￥3500
In-stock
10 mg 現(xiàn)貨 詢價(jià)
50 mg   詢價(jià)  
100 mg   詢價(jià)  

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Customer Review

Other Forms of Delgocitinib:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

查看 JAK 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Delgocitinib (JTE-052) is a specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively[1].

IC50 & Target[1]

JAK2

2.6 nM (IC50)

JAK1

2.8 nM (IC50)

JAK3

13 nM (IC50)

Tyk2

58 nM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.025 μM
Compound: ent-60, JTE-052
Inhibition of JAK1/JAK2 in human A549 assessed as reduction in IL31-induced Stat3 phosphorylation preincubated for 30 mins followed by IL31 stimulation and measured after 15 mins
Inhibition of JAK1/JAK2 in human A549 assessed as reduction in IL31-induced Stat3 phosphorylation preincubated for 30 mins followed by IL31 stimulation and measured after 15 mins
[PMID: 32511913]
PBMC IC50
0.018 μM
Compound: ent-60, JTE-052
Inhibition of JAK1/Tyk2 in human PBMC assessed as reduction in INFalpha-induced Stat1 phosphorylation in CD3+CD4+ cells preincubated for 30 mins followed by INFalpha stimulation and measured after 15 mins
Inhibition of JAK1/Tyk2 in human PBMC assessed as reduction in INFalpha-induced Stat1 phosphorylation in CD3+CD4+ cells preincubated for 30 mins followed by INFalpha stimulation and measured after 15 mins
[PMID: 32511913]
PBMC IC50
0.033 μM
Compound: ent-60, JTE-052
Inhibition of JAK1/JAK2 in human PBMC assessed as reduction in IL6-induced Stat3 phosphorylation in CD3- CD4+ cells preincubated for 30 mins followed by IL6 stimulation and measured after 15 mins
Inhibition of JAK1/JAK2 in human PBMC assessed as reduction in IL6-induced Stat3 phosphorylation in CD3- CD4+ cells preincubated for 30 mins followed by IL6 stimulation and measured after 15 mins
[PMID: 32511913]
PBMC IC50
0.04 μM
Compound: ent-60, JTE-052
Inhibition of JAK1/JAK3 in human PBMC assessed as reduction in IL2-induced Stat5 phosphorylation in CD3+CD4+ cells preincubated for 30 mins followed by IL2 stimulation and measured after 15 mins
Inhibition of JAK1/JAK3 in human PBMC assessed as reduction in IL2-induced Stat5 phosphorylation in CD3+CD4+ cells preincubated for 30 mins followed by IL2 stimulation and measured after 15 mins
[PMID: 32511913]
PBMC IC50
0.084 μM
Compound: ent-60, JTE-052
Inhibition of JAK2/Tyk2 in human PBMC assessed as reduction in IL-23-induced Stat3 phosphorylation in CD3+CD4+ cells preincubated for 30 mins followed by IL-23 stimulation and measured after 15 mins
Inhibition of JAK2/Tyk2 in human PBMC assessed as reduction in IL-23-induced Stat3 phosphorylation in CD3+CD4+ cells preincubated for 30 mins followed by IL-23 stimulation and measured after 15 mins
[PMID: 32511913]
PBMC IC50
0.3 μM
Compound: ent-60, JTE-052
Inhibition of JAK2 in human PBMC assessed as reduction in GM-CSF-induced Stat5 phosphorylation in CD3- CD4+ cells preincubated for 30 mins followed by GM-CSF stimulation and measured after 15 mins
Inhibition of JAK2 in human PBMC assessed as reduction in GM-CSF-induced Stat5 phosphorylation in CD3- CD4+ cells preincubated for 30 mins followed by GM-CSF stimulation and measured after 15 mins
[PMID: 32511913]
Sf21 IC50
0.0026 μM
Compound: ent-60, JTE-052
Inhibition of N-terminal GST-fused human JAK2 (880 to end residues) expressed in baculovirus infected Sf21 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method
Inhibition of N-terminal GST-fused human JAK2 (880 to end residues) expressed in baculovirus infected Sf21 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method
[PMID: 32511913]
Sf9 IC50
0.013 μM
Compound: ent-60, JTE-052
Inhibition of human JAK3 (780 to end residues) expressed in baculovirus infected Sf9 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method
Inhibition of human JAK3 (780 to end residues) expressed in baculovirus infected Sf9 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method
[PMID: 32511913]
T-cell IC50
0.0089 μM
Compound: ent-60, JTE-052
Inhibition of IL2-induced human T cell proliferation preincubated for 30 mins followed by IL2 stimulation and measured after 3 days by [3H]thymidine incorporation based scintillation counting method
Inhibition of IL2-induced human T cell proliferation preincubated for 30 mins followed by IL2 stimulation and measured after 3 days by [3H]thymidine incorporation based scintillation counting method
[PMID: 32511913]
T-cell IC50
8.9 nM
Compound: 17
Inhibition of IL-2 induced human T cell proliferation preincubated with compound for 30 mins followed by IL-2 induction and measured after 3 days in the presence of [3H]thymidine by scintillation counter analysis
Inhibition of IL-2 induced human T cell proliferation preincubated with compound for 30 mins followed by IL-2 induction and measured after 3 days in the presence of [3H]thymidine by scintillation counter analysis
[PMID: 32120325]
體外研究
(In Vitro)

在酶促測(cè)定中，Delgocitinib 有效抑制所有 JAK 亞型，JAK1、JAK2、JAK3 和 Tyk2 的 IC50 值為 2.8±0.6、2.6±0.2、13±0 和 58±9 nM。Lineweaver-Burk 圖顯示，Delgocitinib 對(duì)所有 JAK 的抑制模式與 ATP 競(jìng)爭(zhēng)，JAK1、JAK2 的 Ki 值為 2.1±0.3、1.7±0.0、5.5±0.3 和 14±1 nM，JAK3 和 Tyk2。在這些基于細(xì)胞的細(xì)胞因子信號(hào)轉(zhuǎn)導(dǎo)測(cè)定中，Delgocitinib 抑制由 IL-2、IL-6、IL-23、GM-CSF 和 IFN-α 誘導(dǎo)的 Stat 蛋白磷酸化，IC50 值為分別為 40±9、33±14、84±11、304±22 和 18±3 nM。Delgocitinib 還以濃度依賴性方式抑制 IL-2 誘導(dǎo)的 T 細(xì)胞增殖 (IC50=8.9±3.6 nM)，其效力與 CP-690550 相似 (IC >50=16nM)[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Delgocitinib減少了IFN-γ的產(chǎn)生，但給藥前1小時(shí)的效力高于給藥前6小時(shí)（ED50 = 0.24 mg/kg 對(duì)比 1.3 mg/kg）。從第1天開(kāi)始給藥，Delgocitinib可以預(yù)防后爪腫脹以及炎癥細(xì)胞浸潤(rùn)和滑膜細(xì)胞增生的組織學(xué)變化。Delgocitinib還抑制了放射學(xué)和組織學(xué)上的骨破壞和軟骨破壞。從第15天開(kāi)始給藥，Delgocitinib以劑量依賴性方式減少爪部腫脹。此外，在研究結(jié)束時(shí)的組織學(xué)和放射學(xué)檢查中，Delgocitinib改善了炎癥細(xì)胞浸潤(rùn)、滑膜細(xì)胞增生以及軟骨/骨破壞的情況[1]。

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

310.35

Formula

C16H18N6O
CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

迪高替尼
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 58 mg/mL (186.89 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.2222 mL 16.1108 mL 32.2217 mL
5 mM 0.6444 mL 3.2222 mL 6.4443 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 2.5 mg/mL (8.06 mM); 澄清溶液

  • 方案 二

    請(qǐng)依序添加每種溶劑： 5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.06 mM); 澄清溶液

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.87%

參考文獻(xiàn)
Cell Assay
[1]

For determination of IL-2-induced T cell proliferation, human T cells are precultured with 10 μg/mL PHA-M for 3 days and plated in 96-well plates at 1.0×104 cells/well in the presence or absence of various concentrations of Delgocitinib. Following preincubation with Delgocitinib for 30 min at 37°C, the cells are stimulated by adding 20 ng/mL recombinant human IL-2 to each well and incubated for 3 days at 37°C under 5 % CO2. After completion of the culture period, the cells are harvested with a 96-well harvester and counted in a scintillation counter[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Lewis rats are used in this study. First, collagen-induced arthritis (CIA) is induced in rats. Lewis rats are immunized with 1 mL of the emulsion (1 mg of type II collagen) via ten intradermal injections on the back under anesthesia. The rats are then challenged with 0.2 mL of the emulsion injected into the base of the tail on day 8 under anesthesia. Delgocitinib is given orally once daily from day 1 to day 21 (preventive administration) or from day 15 to day 28 (therapeutic administration). After arthritis induction, the hind paw volume is measured by a water displacement method using a plethysmometer. On day 22 or day 29, the rats are euthanized, and their hind paws are excised and X-rayed or processed for histological evaluation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2222 mL 16.1108 mL 32.2217 mL 80.5542 mL
5 mM 0.6444 mL 3.2222 mL 6.4443 mL 16.1108 mL
10 mM 0.3222 mL 1.6111 mL 3.2222 mL 8.0554 mL
15 mM 0.2148 mL 1.0741 mL 2.1481 mL 5.3703 mL
20 mM 0.1611 mL 0.8055 mL 1.6111 mL 4.0277 mL
25 mM 0.1289 mL 0.6444 mL 1.2889 mL 3.2222 mL
30 mM 0.1074 mL 0.5370 mL 1.0741 mL 2.6851 mL
40 mM 0.0806 mL 0.4028 mL 0.8055 mL 2.0139 mL
50 mM 0.0644 mL 0.3222 mL 0.6444 mL 1.6111 mL
60 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3426 mL
80 mM 0.0403 mL 0.2014 mL 0.4028 mL 1.0069 mL
100 mM 0.0322 mL 0.1611 mL 0.3222 mL 0.8055 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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產(chǎn)品名稱：
Delgocitinib
目錄號(hào)：
HY-109053
需求量：