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

Oclacitinib  (Synonyms: PF-03394197)

目錄號: HY-13577 純度: 99.59%
COA 產(chǎn)品使用指南 技術(shù)支持

Oclacitinib 是一種新型 JAK 抑制劑。Oclacitinib 抑制 JAK1 最有效，IC50 為 10 nM。

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Oclacitinib Chemical Structure

Oclacitinib Chemical Structure

CAS No. : 1208319-26-9

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥605
In-stock
5 mg ￥550
In-stock
10 mg ￥950
In-stock
25 mg ￥1900
In-stock
50 mg ￥3200
In-stock
100 mg ￥5600
In-stock
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Oclacitinib:

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻

查看 JAK 亞型特異性產(chǎn)品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Oclacitinib is a novel JAK inhibitor. Oclacitinib is most potent at inhibiting JAK1 (IC50=10 nM).

IC50 & Target

JAK1

10 nM (IC50)

JAK2

18 nM (IC50)

Tyk2

84 nM (IC50)

JAK3

99 nM (IC50)

體外研究
(In Vitro)

Using isolated enzyme systems and in vitro human or canine cell models, potency and selectivity of Oclacitinib is determined against JAK family members and cytokines that trigger JAK activation in cells. Inhibitory activity of Oclacitinib against JAK family members is determined in isolated enzyme systems. Oclacitinib inhibits JAK1, JAK2, JAK3, and TYK2 by 50% at concentrations (IC50's) of 10, 18, 99, and 84 nM, respectively. Oclacitinib is most potent against the JAK1 enzyme, showing a 1.8-fold selectivity for JAK1 vs. JAK2 and 9.9-fold selectivity toward JAK1 vs. JAK3. Oclacitinib inhibits JAK family members by 50% at concentrations (IC50's) ranging from 10 to 99 nM and does not inhibit a panel of 38 non-JAK kinases (IC50's > 1000 nM). Oclacitinib also inhibits the function of JAK1-dependent cytokines involved in allergy and inflammation (IL-2, IL-4, IL-6, and IL-13) as well as pruritus (IL-31) at IC50's ranging from 36 to 249 nM. Oclacitinib has minimal effects on cytokines that does not activate the JAK1 enzyme in cells (erythropoietin, granulocyte/macrophage colony-stimulating factor, IL-12, IL-23; IC50's > 1000 nM) [1].Topical treatment with Tofacitinib (0.1%) and Oclacitinib (0.1%) leads to significant reduction of cell migration from mouse ear explants compared with vehicle-treated ears (all P < 0.05). The cell counts of MHC class II positive cells (that is, Langerhans cells) are significantly lower in vehicle-treated compared with each JAK inhibitor–treated epidermis (all P < 0.01) [2].

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

Scratching bouts at the high dose in the Oclacitinib group are significantly less than in the vehicle-only group (P<0.01)[2]. Client-owned dogs (n=436) with moderate to severe owner-assessed pruritus and a presumptive diagnosis of allergic dermatitis are enrolled. Dogs are randomized to either Oclacitinib at 0.4-0.6 mg/kg orally twice daily or an excipient-matched placebo. An enhanced 10 cm visual analog scale (VAS) is used to assess the severity of pruritus from day 0 to 7 and to assess the severity of dermatitis on days 0 and 7. Dogs can remain on the study for 28 days. Oclacitinib produces a rapid onset of efficacy within 24 h[3].

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

337.44

Formula

C15H23N5O2S
CAS 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 5 mg/mL (14.82 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.9635 mL 14.8174 mL 29.6349 mL
5 mM 0.5927 mL 2.9635 mL 5.9270 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
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；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.5 mg/mL (1.48 mM); 澄清溶液

    此方案可獲得 ≥ 0.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 5.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% Corn Oil

    Solubility: ≥ 0.5 mg/mL (1.48 mM); 澄清溶液

    此方案可獲得 ≥ 0.5 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。

    以 1 mL 工作液為例，取 100 μL 5.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動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 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，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)給藥周期超過半月以上，請謹慎選擇該方案。
請確保第一步儲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: 99.59%

參考文獻
Kinase Assay
[1]

Recombinant human active kinase domains for JAK1, JAK2, JAK3, and TYK2 are used in isolated enzyme assays using Caliper microfluidics technology to determine potency of Oclacitinib against the JAK family members. Sequence homology to the analogous sequences in the canine JAK enzymes are 98, 98, 100, and 90%, respectively. Invitrogen kinase panel testing is performed to determine potency of Oclacitinib toward 38 different non-JAK kinases using their SelectScreen Kinase Profiling Services. Oclacitinib is evaluated at a concentration of 1 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2][3]

Mice[2]
BALB/cAnN (female, 6 weeks old) are used. The JAK inhibitors (Tofacitinib or Oclacitinib) are administered orally or topically 30 minutes before and 4 hours after toluene-2,4-diisocyanate (TDI) challenge because the absorption of Tofacitinib and Oclacitinib is rapid, with plasma concentrations for both Tofacitinib and Oclacitinib peaking at around 1 hour after oral or intravenous administration. Tofacitinib and Oclacitinib both have a short half-life of 2 and 4 hours after administration, respectively. Each drug is diluted in a 0.5% methylcellulose/0.25% Tween 20 solution for oral administration, and a 7:1 acetone:DMSO solution for topical application to concentrations described subsequently. For each drug, a vehicle-only control group and low- and high-dose groups are set. Oral doses are as follows: Tofacitinib, 10 and 30 mg/kg; and Oclacitinib, 30 and 45 mg/kg. Topically administered doses are 0.1, 0.25, and 0.5% for both chemicals. The oral doses of Tofacitinib and Oclacitinib used in this study are selected.
Dogs[3]
Dogs are randomized to one of two treatment groups (i.e. Oclacitinib or placebo) in a 1:1 ratio. Dogs in the Oclacitinib treatment group are given Oclacitinib maleate caplets orally at a dose of 0.4-0.6 mg/kg twice daily. The scored caplets are provided in three strengths containing 3.6, 5.4 and 16 mg of Oclacitinib. Dogs in the placebo treatment group are given the same number of caplets, identical in appearance to Oclacitinib maleate caplets and containing all of the same excipients except Oclacitinib maleate.

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

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(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 2.9635 mL 14.8174 mL 29.6349 mL 74.0872 mL
5 mM 0.5927 mL 2.9635 mL 5.9270 mL 14.8174 mL
10 mM 0.2963 mL 1.4817 mL 2.9635 mL 7.4087 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：
Oclacitinib
目錄號：
HY-13577
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