SGI-7079 is a novel Axl inhibitor. SGI-7079 decreased IBC cell proliferation, migration and invasion in vitro and inhibited tumor growth of IBC cells in vivo. Mesenchymal cells also expressed increased levels of the receptor tyrosine kinase Axl and showed a trend toward greater sensitivity to the Axl inhibitor SGI-7079, whereas the combination of SGI-7079 with erlotinib reversed erlotinib resistance in mesenchymal lines expressing Axl and in a xenograft model of mesenchymal NSCLC.
|Source||Cancer Res (2013). Figure 6. SGI-7079|
|Cell Lines||SUM149 cells|
|Incubation Time||72 h|
|Results||SGI-7079 treatment inhibited the phosphorylation of Axl at Tyr 702 upon Gas6 stimulation in SUM149 cells|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 60 mg/mL|
 Byers LA, et al. Clin Cancer Res. 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.
|Related Axl Products|
ONO-7475 is a potent and orally active Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively.
TP-0903 is a potent and selective AXL inhibitor with an IC50 value of 27 nM.
R428 is a potent and selective small-molecule inhibitor of Axl kinase with IC50 of 14 nM.
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