AG-490

AG-490 is a member of the tyrphostin family of small molecule inhibitors of tyrosine kinases including EGFR, HER2, JAK2, JAK3, and STAT5a/b 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.   Induces differentiation of mouse. Blocks growth of acute lymphoblastic leukemia pre-B cells by inducing programmed cell death, via inhibition of JAK2. Inhibits proliferation of cervical carcinoma cell lines. Inhibits STAT3 phosphorylation and induced translocation of beta-catenin to the cytoplasm in the colorectal cell line SW480. Induces S phase arrest of GL15 glioblastoma cells via JAK2 inhibition. Inhibits EGF-dependant proliferation of NIH3T3 cell lines. Blocks IL-2 induced thymidine incorporation in T-cell lines.