ATN-161 trifluoroacetate salt 是一种新型整合素 α5β1 拮抗剂,可在小鼠模型中抑制血管生成和肝转移瘤的生长。
产品描述
ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist that inhibits angiogenesis and growth of liver metastases and improves survival in a murine model.
体外活性
The combination of ATN-161 plus 5-FU significantly reduces tumor cell proliferation compared to control and single-agent therapy. Moreover, combination therapy leads to a significant increase of apoptotic (TUNEL-positive) tumor cells, 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 than controls[1]. ATN-161 inhibits 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) [2].
体内活性
The preliminary experiments with α5β1-negative human colon cancer xenografts (HT29) demonstrate that treatment with ATN-161 significantly reduces tumor weight and vessel density [1]. Injection of ATN-161 after laser photocoagulation inhibits choroidal neovascularization (CNV) leakage and neovascularization to an extent similar to AF564 [2].
Cas No.
904763-27-5
分子式
C25H36F3N9O10S
分子量
711.67
别名
ATN-161 TFA salt
储存和溶解度
DMSO:10mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years