SGI 7079 Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml

form 

A crystalline solid

color 

Light yellow to yellow

SGI 7079 Usage And Synthesis

Description

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.

Uses

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.

IC 50

Axl

References

[1] XIAOPING WANG. TIG1 promotes the development and progression of inflammatory breast cancer through activation of Axl kinase.[J]. Cancer research, 2013, 73 21: 6516-6525. DOI: 10.1158/0008-5472.can-13-0967
[2] LAUREN AVERETT BYERS. An epithelial-mesenchymal transition gene signature predicts resistance to EGFR and PI3K inhibitors and identifies Axl as a therapeutic target for overcoming EGFR inhibitor resistance.[J]. Clinical Cancer Research, 2013: 279-290. DOI: 10.1158/1078-0432.ccr-12-1558

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