SRI 31215 是 matriptase、hepsin、肝细胞生长因子激活剂(HGFA)的三重抑制剂，IC50值分别为 0.69 μM、0.65 μM、0.3 μM。它能够阻断 pro-HGF 的活化，模拟 HAI-1/2 的活性。

SRI 31215, a small molecule that acts as a triplex inhibitor of matriptase, hepsin and HGFA and mimics the activity of HAI-1/2, endogenous inhibitors of HGF activation with IC50s of 0.69 μM, 0.65 μM, 0.3 μM,

SRI 31215 inhibits fibroblast-induced MET activation, epithelial-mesenchymal transition and migration of cancer cells.?SRI 31215 overcomes primary resistance to cetuximab and gefitinib in HGF-producing colon cancer cells and prevents fibroblast-mediated resistance to EGFR inhibitors.?Thus, SRI 31215 blocks signaling between cancer cells and fibroblasts and inhibits the tumor-promoting activity of cancer-associated fibroblasts.

DU145 cells were cultured in 6-well tissue culture plates at a density of 1 103 cells per well.?After colonies formed (6-8 days), cells were serum-starved overnight and were then treated with recombinant HGF (10 ng/ml) or with conditioned media from 18Co fibroblasts in the presence or absence of SRI 31215 (10 μM) or the MET kinase inhibitor JNJ 38877605 (1 μM) for 24 hours.?Cells were washed with PBS and colonies were fixed and stained with 0.5% crystal violet solution in 6% glutaraldehyde.

1832686-44-8

C29H35F6N5O5

647.619

SRI 31215

DMSO:Soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years