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

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.

For research use only. We do not sell to patients.

IRAK1-IN-2

IRAK1-IN-2 Chemical Structure

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Description

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

 

In Vivo

IRAK1-IN-2 (compound 34) (20-40 mg/kg; p.o.; once daily; 16 days) dose-dependently inhibits hepatocellular carcinoma xenograft tumor growth in BALB/c nude mice, with a favorable safety profile and suppression of IRAK1/STAT3 signaling in tumor tissue[1].

MedChemExpress (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.
Molecular Weight

554.56

Formula

C29H29F3N4O4

SMILES

O=C1C=CC(C2=CC(C(F)(F)F)=CC=C2)=NN1CCOC3=C4C=CC(OCCCN5CCOCC5)=CC4=NC=C3

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
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    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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Product Name:
IRAK1-IN-2
Cat. No.:
HY-181712
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