2. Protein Tyrosine Kinase/RTK
  3. Itk
  4. GNE-9822

GNE-9822 是一种口服有效的选择性的 ITK 抑制剂，Ki=0.7 nM，EC50=354.5 nM。GNE-9822 具有良好的 ADME 特性。GNE-9822 可用于哮喘的研究。

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GNE-9822 Chemical Structure

GNE-9822 Chemical Structure

CAS No. : 1557232-32-2

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规格 价格 是否有货 数量
1 mg ￥2160
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5 mg ￥5400
In-stock
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100 mg   询价  

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Customer Review

GNE-9822 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki value of 0.7 nM, and an EC50 value of 354.5 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma[1][2].

IC50 & Target

EC50: 354.5 nM (ITK)[2]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Jurkat IC50
0.045 μM
Compound: 1, GNE-9822
Inhibition of ITK in TCR stimulated human Jurkat T cells assessed as reduction of PLC-gamma phosphorylation preincubated for 30 mins followed by TCR induction for 2 mins
Inhibition of ITK in TCR stimulated human Jurkat T cells assessed as reduction of PLC-gamma phosphorylation preincubated for 30 mins followed by TCR induction for 2 mins
[PMID: 25844760]
Jurkat IC50
4.7 μM
Compound: 1, GNE-9822
Cytotoxicity against human Jurkat T cells without TCR stimulation assessed as cell viability by ATPlite assay
Cytotoxicity against human Jurkat T cells without TCR stimulation assessed as cell viability by ATPlite assay
[PMID: 25844760]
Jurkat IC50
55 nM
Compound: 28
Inhibition of ITK in human Jurkat cells assessed as reduction in PLC-gamma phosphorylation after 30 mins
Inhibition of ITK in human Jurkat cells assessed as reduction in PLC-gamma phosphorylation after 30 mins
[PMID: 24918870]
体外研究
(In Vitro)

GNE-9822 (compound 28) 抑制 PLCγ 的磷酸化，IC50 值为 55 nM[1]。

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

GNE-9822 相关抗体:
体内研究
(In Vivo)

GNE-9822 (compound 28; po and iv; 1 and 5 mg/kg) 在小鼠和大鼠中观察到良好的生物利用度和半衰期[1]。

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

Animal Model: BALB/c mouse and Sprague-Dawley rats[1]
Dosage: 1 and 5 mg/kg
Administration: po (5 mg/kg) and iv (1 mg/kg)
Result: 1.19
species route dose volume (mL/kg) dose (mg/kg) Cmax (μM) AUC (μM·h) Cl (mL/min/kg) T1/2 (h) Vss (L/kg) %F
mouse (BALB/c) IV 1.0 1.0 1.5 40 2.9 10
mouse (BALB/c) PO 5.0 50 3.8 2.7 36
Animal Model: BALB/c mouse and Sprague-Dawley rats[1]
Dosage: 1 and 5 mg/kg
Administration: po (5 mg/kg) and iv (1 mg/kg)
Result: 1.19
species route dose volume (mL/kg) dose (mg/kg) Cmax (μM) AUC (μM·h) Cl (mL/min/kg) T1/2 (h) Vss (L/kg) %F
rat (Sprague-Dawley IV 1.0 1.0 0.6 70 3.0 14
rat (Sprague-Dawley PO 2.0 5.0 0.2 1.1 40
分子量

420.55

Formula

C24H32N6O
CAS 号
性状

固体

颜色

Off-white to light yellow

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 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 62.5 mg/mL (148.61 mM; 超声助溶; 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 2.3778 mL 11.8892 mL 23.7784 mL
5 mM 0.4756 mL 2.3778 mL 4.7557 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。-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

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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

GNE-9822 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, 6 months; -20°C, 1 month。-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 2.3778 mL 11.8892 mL 23.7784 mL 59.4460 mL
5 mM 0.4756 mL 2.3778 mL 4.7557 mL 11.8892 mL
10 mM 0.2378 mL 1.1889 mL 2.3778 mL 5.9446 mL
15 mM 0.1585 mL 0.7926 mL 1.5852 mL 3.9631 mL
20 mM 0.1189 mL 0.5945 mL 1.1889 mL 2.9723 mL
25 mM 0.0951 mL 0.4756 mL 0.9511 mL 2.3778 mL
30 mM 0.0793 mL 0.3963 mL 0.7926 mL 1.9815 mL
40 mM 0.0594 mL 0.2972 mL 0.5945 mL 1.4861 mL
50 mM 0.0476 mL 0.2378 mL 0.4756 mL 1.1889 mL
60 mM 0.0396 mL 0.1982 mL 0.3963 mL 0.9908 mL
80 mM 0.0297 mL 0.1486 mL 0.2972 mL 0.7431 mL
100 mM 0.0238 mL 0.1189 mL 0.2378 mL 0.5945 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:

GNE-98221557232-32-2GNE9822GNE 9822ItkInterleukin-2 inducible T-cell kinaseIL2 inducible T-cell kinasephosphorylationPLCγbioavailabilityhalflivesorally activeInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-12410
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