2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt Immunology/Inflammation
  3. JAK IFNAR
  4. TYK2-IN-12

TYK2-IN-12 (compound 30) 是一种口服有效的和选择性的 TYK2 (酪氨酸激酶 2) 抑制剂，Ki 为 0.51 nM。TYK2-IN-12 分别抑制 IL-12 诱导的人和小鼠全血中 IFNγ，IC50 值分别为 2.7 和 7.0 μM。TYK2-IN-12 可用于银屑病研究。

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TYK2-IN-12 Chemical Structure

TYK2-IN-12 Chemical Structure

CAS No. : 2244061-66-1

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规格 价格 是否有货 数量
5 mg ￥770
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10 mg ￥1225
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Customer Review

TYK2-IN-12 相关抗体

Top Publications Citing Use of Products

查看 JAK 亚型特异性产品:

查看所有亚型
JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TYK2-IN-12 (compound 30) is an orally active, potent and selective TYK2 (tyrosine kinase 2) inhibitor, with a Ki of 0.51 nM. TYK2-IN-12 inhibits IL-12 induced IFNγ, with IC50 values of 2.7 and 7.0 μM in human and mouse whole blood, respectively. TYK2-IN-12 can be used for psoriasis research[1].

IC50 & Target

Tyk2

0.51 nM (Ki)

JAK3

6.63 nM (Ki)

JAK2

21.93 nM (Ki)

JAK1

45.9 nM (Ki)

体外研究
(In Vitro)

TYK2-IN-12 (compound 30) shows 90, 43, and 13-fold selectivity over JAK1, JAK2, and JAK3, respectively[1].
TYK2-IN-12 exhibits excellent selectivity over hERG (IC50 > 30 μM) and over a panel of 10 cytochrome P450 enzymes (IC50s > 30 μM against CYP450s 3A4, 3D6, 2C9, 2C8, 1A2, 2A6, 2B6, 2C19, 2E1, and 3A5)[1].
TYK2-IN-12 shows cell-based potency and selectivity in human PBMC by blockade of IL-12 induced phospho-STAT4, GM-CSF induced phospho-STAT5, and IL-2 induced phospho-STAT5, with IC50 values of 0.10 μM, 4.1 μM and 0.25 μM, respectively[1].

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

TYK2-IN-12 相关抗体:
体内研究
(In Vivo)

TYK2-IN-12 (compound 30) (0-100 mg/kg, PO, daily for 10 days) dose-dependently reduces immune responses[1].
TYK2-IN-12 (3 mg/kg (IV), 10 mg/kg (PO), once) shows moderate clearance and volumes of distribution, and exhibits moderate to good oral absorption[1].
Pharmacokinetic Parameters of TYK2-IN-12 in male C57Bl/6 mice and smale Sprague-Dawley rats[1].

Species Mouse Rat
PPB Fumax (h) 0.061 0.10
CL (mL/min/kg) 28 27
t1/2 (h) 1.8 1.6
Vd (L/kg) 1.2 1.9
F (%) >90 32

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

Animal Model: C57BL/6 mice (IL-23 induced inflammation model)[1]
Dosage: 0, 10, 30, and 100 mg/kg
Administration: PO, daily for 10 days
Result: Dose-dependently reduced immune responses, with up to 74 % inhibition of ear swelling and 96 % inhibition of tissue levels of IL-17A at 100 mg/kg, highlighting the crucial role of TYK2 in IL-23 induced IL-17 and tissue inflammation. Exhibited improved skin histology and a dose-dependent reduction of spleen weight.
Animal Model: Male C57Bl/6 mice, male SD rats[1]
Dosage: 3 mg/kg (IV), 10 mg/kg (PO)
Administration: IV or PO, once (Pharmacokinetic Analysis)
Result: Showed moderate clearance and volumes of distribution of 1.2 L/Kg and 1.9 L/Kg, respectively in mouse and rat IV PK, and exhibited moderate to good oral absorption, with oral bioavailabilities of 32-100%.
分子量

434.44

Formula

C24H20F2N4O2
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

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 7.14 mg/mL (16.43 mM; 超声助溶 (<60°C); 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 2.3018 mL 11.5091 mL 23.0181 mL
5 mM 0.4604 mL 2.3018 mL 4.6036 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 (sealed storage, away from moisture)。-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

纯度: 98.81%

COA (292 KB) HNMR (262 KB) LCMS (95 KB)

产品使用指南 (1538 KB)
参考文献

TYK2-IN-12 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 (sealed storage, away from moisture)。-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 2.3018 mL 11.5091 mL 23.0181 mL 57.5453 mL
5 mM 0.4604 mL 2.3018 mL 4.6036 mL 11.5091 mL
10 mM 0.2302 mL 1.1509 mL 2.3018 mL 5.7545 mL
15 mM 0.1535 mL 0.7673 mL 1.5345 mL 3.8364 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:

TYK2-IN-122244061-66-1JAKIFNARJanus kinaseInterferon-α/β receptorInterferon-alpha/beta receptorPsoriasisPyrrolidino-pyridinePyrrolidino-pyrimidineFEPPBMCIL12pSTAT4Inhibitorinhibitorinhibit

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