AG-490

AG-490 is a member of the tyrphostin family of small molecule inhibitors of tyrosine kinases including EGFR (Gazit et al.), HER2 (Gazit et al.), JAK2 (Burger et al.), JAK3 (Brown et al.), and STAT5a/b (Wang et al.) with IC₅₀ values of 0.1, 13.5, 11 and 12 μM, respectively. AG-490 does not inhibit LCK, LYN, BTK, SYK, or SRC tyrosine kinases (Meydan et al.).

DIFFERENTIATION

• Induces differentiation of mouse (OG2) embryonic stem cells, with LIF and BMP4 (Chen et al.).

CANCER RESEARCH

• Blocks growth of acute lymphoblastic leukemia pre-B cells by inducing programmed cell death, via inhibition of JAK2 (Meydan et al.).
• Inhibits proliferation of cervical carcinoma cell lines (Soto-Cruz et al.).
• Inhibits STAT3 phosphorylation and induced translocation of beta-catenin to the cytoplasm in the colorectal cell line SW480 (Kawada et al.).
• Induces S phase arrest of GL15 glioblastoma cells via JAK2 inhibition (Sciaccaluga et al.).
• Inhibits EGF-dependant proliferation of NIH3T3 cell lines (Gazit et al.).
• Blocks IL-2 induced thymidine incorporation in T-cell lines (Wang et al.).