CAS NO: | 904763-27-5 |
生物活性 | ATN-161 trifluoroacetate salt is a novelintegrinα5β1antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model. | ||||||||||||||||
IC50& Target | Integrin α5β1[1] | ||||||||||||||||
体外研究 (In Vitro) | The 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)[1]. 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)[2]. | ||||||||||||||||
体内研究 (In Vivo) | The preliminary experiments with α5β1-negative human colon cancer xenografts (HT29) show 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]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 711.67 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C25H36F3N9O10S | ||||||||||||||||
CAS 号 | 904763-27-5 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: H2O : 5 mg/mL(7.03 mM;ultrasonic and warming and heat to 60℃) DMSO : 1 mg/mL(1.41 mM;Need ultrasonic) 配制储备液
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