tlrl-gef Gefitinib

RIP2 tyrosine kinase inhibitor (Iressa)

Gefitinib (also known as Iressa) is a selective inhibitor of epidermal growth factor (EGFR), a growth factor that plays a pivotal role in the control of cell growth, apoptosis, and angiogenesis.

EGFR activation stimulates many complex intracellular signaling pathways, primarily the MEK/ERK and PI3K/AKT pathways [1, 2]. Following EGFR activation, Src tyrosine kinases and STAT downstream signaling have also been well documented [2].

Recent studies demonstrated that Gefitinib can inhibit NOD2-induced cytokine release and NF-kB activation by inhibiting RIP2 (receptor-interacting protein 2) tyrosine phophorylation which is critical for activation of NOD2 downsream signaling pathways [3].

 

1. Okamoto K. et al., 2010. Role of survivin in EGFR inhibitor-induced apoptosis in non-small cell lung cancers positive for EGFR mutations. Cancer Res. 70(24):10402-10.
2. Wheeler D. et al., 2010. Understanding resistance to EGFR inhibitors—impact on future treatment strategies. Nat Rev Clin Oncol. 7(9):493-507.
3. Tigno-Aranjuez J. et al., 2010. Inhibition of RIP2’s tyrosine kinase activity limits NOD2-driven cytokine responses. Genes Dev. 24(23):2666-77.

Specifications

Working concentration: 0.1 - 20 µM

Purity: ≥98% (UHPLC)

Solubility: 100 mM in DMSO

CAS number: 184475-35-2

Molecular weight: 446.9

Contents

Gefitinib is provided as a translucent film.

•  10 mg Gefitinib

Gefitinib is shipped at room temperature.

Store at -20°C.

Solid product is stable for 1 year at -20°C when properly stored.

Citations

2017 Sci Rep. 7:40847.

Targeting the miR-200c/LIN28B axis in acquired EGFR-TKI resistance non-small cell lung cancer cells harboring EMT features

Sato H. et al.

2017 Life Sci. 191:180-185.

Gefitinib and pyrrolidine dithiocarbamate decrease viral replication and cytokine production in dengue virus infected human monocyte cultures.

Duran A. et al.

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