SGI 7079

SGI-7079 is an inhibitor of the receptor tyrosine kinase Axl. It inhibits proliferation of inflammatory breast cancer cells (IC₅₀s = 0.43 and 0.15 μM for SUM149 and KPL-4 cells, respectively), decreases invasion, and halts the cell cycle in the G₁ phase. SGI-7079 synergistically increases the potency of erlotinib on EGFR inhibition. In a mouse xenograft model of non-small cell lung cancer, SGI-7079 dose-dependently inhibits tumor growth, an effect that is greater when used in combination with erlotinib.

3-[2-[[3-Fluoro-4-(4-methyl-1-piperazinyl)phenyl]amino]-5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]benzeneacetonitrile is an anticancer agent and a selective Axl inhibitor.