SGI-7079 (C007B-272606)

InformationSGI-7079 SGI-7079, a novel selective Axl inhibitor with an IC50 of 58 nM in vitro, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance.TargetsMet ; Mer ; YES ; RET ; FLT3 16051,;In vitroSGI-7079 exhibits a Ki = 5.7 nM for AXL and inhibits Gas6 ligand-induced tyrosine phosphorylation of human AXL expressed in HEK293T cells (EC50 = 100 nM). It inhibits TAM family members MER and Tyro3 similarly as AXL, and shows potent, low nM inhibition of Syk, Flt1, Flt3, Jak2, TrkA, TrkB, PDGFRβ and Ret kinases. Mesenchymal cells express increased levels of the receptor tyrosine kinase Axl and show a trend toward greater sensitivity to the Axl inhibitor SGI-7079.In vivoSGI-7079 inhibits tumor growth in a dose-dependent manner, and at the maximum dose, inhibits tumor growth by 67%, compared with control. the combination of SGI-7079 with erlotinib reverses erlotinib resistance in mesenchymal lines expressing Axl and in a xenograft model of mesenchymal NSCLC.Cell Research(from reference)Cell lines：HEK-293 cells Concentrations：0.03, 0.1, 0.3, 1, 3 μmol/L Incubation Time：10 min.

Specifications and Purity: ≥98%

Molecular Formula: C26H26FN7

Molecular Weight: 455.53

PubChem CID: 46870258

Isomeric SMILES: CC1=CNC2=NC(=NC(=C12)C3=CC=CC(=C3)CC#N)NC4=CC(=C(C=C4)N5CCN(CC5)C)F

Related Documents: https://aladdin-for-icloud-store.oss-cn-hangzhou.aliyuncs.com/aladdinsci/pdp/sds/1/S413852-SCI_e3f08f6150285d8dbc3d1c43ccb0e80f.pdf