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.
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||91 mg/mL in DMSO|
|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|
TIG1 Promotes the Development and Progression of Inflammatory Breast Cancer through Activation of Axl Kinase.
Wang X, et al. Cancer Res. 2013 Sep 6. PMID: 24014597.
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.
Byers LA, et al. Clin Cancer Res. 2013 Jan 1;19(1):279-90. PMID: 23091115.
|Related Axl Products|
R428 is a potent and selective small-molecule inhibitor of Axl kinase with IC50 of 14 nM.
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