中文名称: | ATN-161 trifluoroacetate salt | ||||
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英文名称: | ATN-161 trifluoroacetate salt | ||||
别名: | ATN-161 TFA salt | ||||
CAS No: | 904763-27-5 | 分子式: | C25H36F3N9O10S | 分子量: | 711.67 |
CAS No: | 904763-27-5 | ||||
分子式: | C25H36F3N9O10S | ||||
分子量: | 711.67 |
基本信息
产品编号:A11388 |
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产品名称:ATN-161 trifluoroacetate salt |
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CAS: |
904763-27-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
711.67 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
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Ethanol |
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Water |
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体内(现配现用) |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
1.4051mL |
7.0257mL |
14.0515mL |
5mM |
0.2810mL |
1.4051mL |
2.8103mL |
10mM |
0.1405mL |
0.7026mL |
1.4051mL |
生物活性
产品描述 |
一种新型 integrin α5β1 拮抗剂,在肝转移模型小鼠模型中,抑制血管生成。 |
靶点/IC50 |
Integrin α5β1 |
体外研究 |
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 100nM (P<0.001 vs. VEGF group). |
体内研究 |
The 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. |
推荐实验方法(仅供参考)
细胞实验: |
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Ninety-six well microtiter plates are coated with fibronectin(20μg/mL) overnight at 4℃. HUVECs are then trypsinized as described above and resuspended in 1% FBS-MEM for cell counting. Cell suspensions with 10,000 cells/mL are prepared in serum-reduced conditions by using 1% FBS-MEM, or 1% FBS-MEM containing either ATN-161 (1μM) or ATN-163 (scrambled peptide as control; 1μM) to allow interference by the peptide during the ligand binding process (i.e.,binding of α5β1 to fibronectin). Cells are thereafter plated into each well (2,000 cells/well in 200μL) of the fibronectin-coated 96-well plates.Cells are incubated at 37℃ for 48 hr under these serum-reduced conditions in order to evaluate effects of ATN-161 on EC survival and proliferation.Estimation of cell number is performed by adding 40μL MTT to each well and incubating for 2 hr at 37℃. Media is then removed, cells are solubilized in 100μL DMSO and optical density is measured at 560nm. Experiments are performed in triplicate. |
动物实验: |
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Mice Eight-week-old male BALB/c mice are acclimated for 1 week while caged in groups of 5. Mice are fed a diet of animal chow and water ad libitum throughout the experiment. CT-26 cells (10,000 cells in 50μL HBSS) are injected into the spleens of 40 BALB/c mice to produce liver metastases. Mice are randomly assigned to 1 of 4 treatment groups (10 mice per group): (A) control (saline/saline), (B) 5-FU alone,(C) ATN-161 alone and (D) ATN-161 plus 5-FU. Body weight at randomization is similar among groups. Treatment with ATN-161 (100mg/kg) or saline is started on day 4 after CT-26-cell injection and is administered every third day thereafter by intraperitoneal injection.In previous studies, administration of the peptide every third day has been shown to be adequate for sustained inhibition of integrin α5β1 activity. Mice are allowed to recover for 1 week from the surgical procedure and effects of anesthesia with pentobarbital (Nembutal, 50mg/kg). On day 7, mice are anaesthetized again and osmotic pumps. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )