ATN-161 trifluoroacetate salt (C09-1101-461)

ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.In VitroThe combination of ATN-161 plus 5-FU significantly reduces tumor cell proliferation compared to control and single-agent therapy (p<0.01). In addition, combination therapy leads to a significant increase of apoptotic (TUNEL-positive) tumor cells (p<0.03), whereas single-agent therapy does not increase in TUNEL-positive tumor cells. ATN-161 treatment leads to a significant reduction in EC number (21% decrease) after a 48 hr incubation time compared to control (p<0.03). ATN-161 inhibites VEGF-induced migration and capillary tube formation in hCECs, but did not inhibit proliferation. ATN-161 decreases the number of cells migrating in response to VEGF in a dose-dependent manner starting at 100 nM (P<0.001 vs. VEGF group). MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoThe preliminary experiments with α5β1-negative human colon cancer xenografts (HT29) show that treatment with ATN-161 significantly reduces tumor weight and vessel density . Injection of ATN-161 after laser photocoagulation inhibits choroidal neovascularization (CNV) leakage and neovascularization to an extent similar to AF564. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:Integrin α5β1. Specifications and Purity: ≥95.0%. Molecular Formula: C25H36F3N9O10S. Molecular Weight: 711.67. PubChem CID: 92044380. Isomeric SMILES: CC(=O)N1CCC[C@H]1C(=O)N[C@@H](CC2=CN=CN2)C(=O)N[C@@H](CO)C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(=O)N)C(=O)N.C(=O)(C(F)(F)F)O.