2. Protein Tyrosine Kinase/RTK
  3. Itk
  4. PRN694

PRN694 是一种不可逆的，高效选择性的，有效共价结合的白介素 2 诱导细胞激酶 ITK、 静息淋巴细胞激酶 RLK 双重抑制剂，抑制 ITK、RLK 的IC50 分别为 0.3 nM 和 1.4 nM。PRN694 延长靶向停留时间，使效应细胞在体内外持久衰减。

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PRN694 Chemical Structure

PRN694 Chemical Structure

CAS No. : 1575818-46-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥10525
In-stock
1 mg ￥2800
In-stock
5 mg 现货 询价
10 mg 现货 询价
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PRN694 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC50s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo[1].

IC50 & Target

IC50: 0.3 nM (ITK), 1.4 nM (RLK), 3.3 nM (TEC), 17 nM (BTK), 17 nM (BMX), 30 nM (JAK3), 125 nM (BLK)[1]
体外研究
(In Vitro)

PRN694 inhibits TEC, BTK, BMX, BLK, JAK3 with IC50s of 3.3, 17, 17, 125, 30 nM, respectively[1].
? Immunoblot analysis of TCR activation pathways reveales that PRN694 blocks activation or nuclear translocation of NFAT1, JunB, pIκBα, and pERK. Results reveal inhibition of Ca2+ signaling with PRN694 at all concentrations above 1 nM. PRN694 significantly attenuates NK cell FcR-induced killing at concentrations exceeding 0.37 μM[1].
? Day 6 flow cytometry analysis reveals that PRN694 significantly inhibits the anti-CD3/CD28-induced proliferation of both CD4 and CD8 T-cells (p<0.01)[1].

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

PRN694 相关抗体:
体内研究
(In Vivo)

The PRN694 occupancy of ITK is 98, 95, and 54% at 1, 6, and 14 h, respectively. The concentrations of PRN694 in the plasma are 2.8, 0.66, and 0.027 μM at 1, 6, and 14 h, respectively. At 14 h, the plasma level of PRN694 is over 10 fold lower than the IC50 in whole blood. RN694 treatment also results in significantly lower weights relative to vehicle (p<0.05)[1].
? Colitis studies show reduced numbers of CD4+ T cells present in the colonic epithelium of PRN694-treated mice compare with controls[2].

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

543.67

Formula

C28H35F2N5O2S
CAS 号
性状

固体

颜色

Off-white to light brown

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 125 mg/mL (229.92 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8394 mL 9.1968 mL 18.3935 mL
5 mM 0.3679 mL 1.8394 mL 3.6787 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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

动物实验：

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: ≥ 2.08 mg/mL (3.83 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (3.83 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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

只
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）。
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: ≥99.0%

COA (194 KB) HNMR (100 KB)

产品使用指南 (1538 KB)
参考文献
Kinase Assay
[1]

Recombinant ITK at a final concentration of 0.5 μM in 50 mM Hepes, pH 7.5, 10 mM MgCl2, 0.01% Triton X-100, and 1 mM EGTA are combined with 1.5 μM PRN694 for 90 min to facilitate binding. The mixture is then diluted 50 fold to initiate dissociating of the ligand from the enzyme, and 10 μL is transferred to a Greiner 384-well black plate. Europium-coupled anti-His6 antibody is added to each well and incubated for 5 min, followed by the addition of an ITK binding fluorescent tracer. The tracer binds to ITK as a function of ligand dissociation, and binding is detected by time-resolved FRET between the europium-coupled antibody and the tracer on a plate reader. Time points acquired are 0.25, 1, 3, 6, and 24 h[1].

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

Cells are cultured in vitro at 37°C and 5% CO2 using RPMI 1640 with 10% fetal calf serum. Cells are pretreated for 30 min with PRN694 or other inhibitors and then washed two times. T-cells are then stimulated for 6 h with 1 μg/mL soluble anti-CD3 for CD69 activation, which is detected by flow cytometry, or 45 min with plate-bound anti-CD3 (10 μg/mL plating concentration) and soluble anti-CD28 (1 μg/mL) for downstream signal analysis by immunoblotting. NK cells are stimulated for 6 h with plate-bound anti-CD52 for CD107a/b activation, detected by flow cytometry, or for 45 min for downstream signal analysis by immunoblotting[1].

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

Mice are randomized by weight and sensitized with aliquots of 150 μL of 5% oxazolone in 3 parts ethanol and 1 part acetone on their shaved abdomens. Seven days after the sensitization, the mice are challenged with 10 μL of 3% oxazolone on the front and back of the right ears. The left ears are treated with the ethanol/acetone mixture. One hour prior to the challenge, the animals received either vehicle control (5% ethanol, 95% Captex 355 NP/EF, intraperitoneal injection at 5 mL/kg), 20 mg/kg PRN694 in 5% ethanol, 95% Captex (intraperitoneal injection at 5 mL/kg), or 0.5 mg/kg dexamethasone (intraperitoneal injection at 5 mL/kg). A control group of animals receive no oxazolone or drug treatment. Twenty-four hours after the oxazolone challenge, the mice are sacrificed, and a 7 mm disc is punched out of each ear and weighed to measure edema[1].

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

PRN694 相关分类

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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8394 mL 9.1968 mL 18.3935 mL 45.9838 mL
5 mM 0.3679 mL 1.8394 mL 3.6787 mL 9.1968 mL
10 mM 0.1839 mL 0.9197 mL 1.8394 mL 4.5984 mL
15 mM 0.1226 mL 0.6131 mL 1.2262 mL 3.0656 mL
20 mM 0.0920 mL 0.4598 mL 0.9197 mL 2.2992 mL
25 mM 0.0736 mL 0.3679 mL 0.7357 mL 1.8394 mL
30 mM 0.0613 mL 0.3066 mL 0.6131 mL 1.5328 mL
40 mM 0.0460 mL 0.2299 mL 0.4598 mL 1.1496 mL
50 mM 0.0368 mL 0.1839 mL 0.3679 mL 0.9197 mL
60 mM 0.0307 mL 0.1533 mL 0.3066 mL 0.7664 mL
80 mM 0.0230 mL 0.1150 mL 0.2299 mL 0.5748 mL
100 mM 0.0184 mL 0.0920 mL 0.1839 mL 0.4598 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.

Keywords:

PRN6941575818-46-0PRN 694PRN-694ItkInterleukin-2 inducible T-cell kinaseIL2 inducible T-cell kinaseInhibitorinhibitorinhibit

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