ATN-161 is a five-amino-acid peptide derived from the synergy region of fibronectin and a beta integrin antagonist with antitumor activity.
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产品名称 | Integrin ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tirofiban | ✔ | 99%+ | |||||||||||||||||
ATN-161 | ✔ | 98% | |||||||||||||||||
RGD | ✔ | 98% | |||||||||||||||||
A-205804 |
++
ICAM-1, IC50: 25 nM E-selectin, IC50: 20 nM |
98% | |||||||||||||||||
SB-273005 |
++++
αvβ3 receptor, IC50: 1.2 nM αvβ5 receptor, IC50: 0.3 nM |
98+% | |||||||||||||||||
Lifitegrast | ✔ | 97% | |||||||||||||||||
Cilengitide TFA |
+++
αvβ3 receptor, IC50: 4.1 nM αvβ5 receptor, IC50: 79 nM |
99%+ | |||||||||||||||||
Cyclo(-RGDfK) TFA | ✔ | 99%+ | |||||||||||||||||
Cyclo(RGDyK) trifluoroacetate |
++
αVβ3 integrin, IC50: 20 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | The combination of ATN-161 and 5-FU results in a notable reduction in tumor cell proliferation compared to both control and monotherapy (p<0.01). Furthermore, the combined treatment leads to a significant increase in apoptotic (TUNEL-positive) tumor cells (p<0.03), whereas monotherapy does not increase the number of TUNEL-positive tumor cells. Following a 48-hour incubation period, ATN-161 treatment leads to a significant decrease in endothelial cell (EC) count (21% reduction) compared to control (p<0.03) [1]. ATN-161 inhibits VEGF-induced migration and capillary tube formation in hCECs, while showing no effect on proliferation. It reduces 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 | Preliminary experiments conducted with α5β1-negative human colon cancer xenografts (HT29) demonstrate that ATN-161 treatment significantly decreases both tumor weight and vessel density [1]. Administration of ATN-161 following laser photocoagulation effectively suppresses choroidal neovascularization (CNV) leakage and neovascularization to a degree comparable to that of AF564 [2]. |
体外研究 | The combination of ATN-161 and 5-FU results in a notable reduction in tumor cell proliferation compared to both control and monotherapy (p<0.01). Furthermore, the combined treatment leads to a significant increase in apoptotic (TUNEL-positive) tumor cells (p<0.03), whereas monotherapy does not increase the number of TUNEL-positive tumor cells. Following a 48-hour incubation period, ATN-161 treatment leads to a significant decrease in endothelial cell (EC) count (21% reduction) compared to control (p<0.03) [1]. ATN-161 inhibits VEGF-induced migration and capillary tube formation in hCECs, while showing no effect on proliferation. It reduces 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]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.67mL 0.33mL 0.17mL |
8.37mL 1.67mL 0.84mL |
16.73mL 3.35mL 1.67mL |
CAS号 | 262438-43-7 |
分子式 | C23H35N9O8S |
分子量 | 597.64 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
溶解度 | |
动物实验配方 |