1. Immunology/Inflammation
  2. IRAK
  3. IRAK1-IN-2

IRAK1-IN-2 是一种口服有效的 IRAK1 抑制剂和抗肿瘤剂,对 IRAK4 和同组其他激酶具有高选择性。IRAK1-IN-2 能够功能性抑制 IRAK1,干扰 TLR/IL-1R 信号通路。IRAK1-IN-2 可在体外和动物模型中抑制肝细胞癌相关细胞过程。IRAK1-IN-2 可作为 IRAK1 研究的化学探针,用于肝细胞癌的研究。

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IRAK1-IN-2

IRAK1-IN-2 Chemical Structure

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查看 IRAK 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IRAK1-IN-2 is an orally active IRAK1 inhibitor and antitumor agent with high selectivity for IRAK4 and other kinases in the same group. IRAK1-IN-2 functionally inhibits IRAK1 and interferes with the TLR/IL-1R signaling pathway. IRAK1-IN-2 suppresses hepatocellular carcinoma-related cellular processes in vitro and in animal models. IRAK1-IN-2 serves as a chemical probe for IRAK1 research and is applicable to studies on hepatocellular carcinoma[1].

IC50 & Target

IRAK1

 

体内研究
(In Vivo)

IRAK1-IN-2 (compound 34) (20-40 mg/kg; p.o.; 每日 1 次, 16 d) 可剂量依赖性地抑制 BALB/c 裸鼠中肝细胞癌异种移植瘤的生长,具有良好的安全性,并可抑制肿瘤组织中的 IRAK1/STAT3 信号通路[1]

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

Animal Model: BALB/c nude mice with Hepatocellular carcinoma[1]
Dosage: 20 mg/kg; 40 mg/kg
Administration: p.o.; once daily; 16 days
Result: Achieved a 51.1% tumor growth inhibition rate at 20 mg/kg.
Achieved a 70.3% tumor growth inhibition rate at 40 mg/kg.
Showed no significant differences in body weight between treatment groups and controls during the study period.
Significantly reduced levels of phosphorylated IRAK1 and phosphorylated STAT3 in harvested tumor tissue.
Revealed no obvious pathological lesions in major organs at either dose.
分子量

554.56

Formula

C29H29F3N4O4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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产品名称:
IRAK1-IN-2
目录号:
HY-181712
需求量: