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  2. Integrin
  3. ATN-161 trifluoroacetate salt

ATN-161 trifluoroacetate salt  (Synonyms: ATN-161 TFA salt)

目录号: HY-13535A 纯度: ≥95.0%
COA 产品使用指南

ATN-161 trifluoroacetate salt 是一种新型 integrin α5β1 拮抗剂,在肝转移模型小鼠模型中,抑制血管生成。

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ATN-161 trifluoroacetate salt Chemical Structure

ATN-161 trifluoroacetate salt Chemical Structure

CAS No. : 904763-27-5

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Other Forms of ATN-161 trifluoroacetate salt:

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.

IC50 & Target

Integrin α5β1[1]

体外研究
(In Vitro)

与对照和单一药物处理相比,ATN-161 trifluoroacetate salt 加 5-FU 的组合显著降低了肿瘤细胞增殖 (p<0.01)。此外,联合处理导致凋亡 (TUNEL 阳性) 肿瘤细胞显著增加 (p<0.03),而单一药物处理不会增加 TUNEL 阳性肿瘤细胞。与对照相比,孵育 48 小时后,ATN-161 trifluoroacetate salt 处理导致 EC 数量显著减少 (减少 21%) (p<0.03)[1]。ATN-161 trifluoroacetate salt 抑制 VEGF 诱导的 hCEC 迁移和毛细管形成,但不抑制增殖。从 100 nM 开始,ATN-161 trifluoroacetate salt 以剂量依赖性方式减少响应 VEGF 的细胞迁移数量 (P<0.001 与 VEGF 组相比)[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

α5β1 阴性人结肠癌异种移植物 (HT29) 的初步实验表明,用 ATN-161 trifluoroacetate salt 处理可显著降低肿瘤重量和血管密度[1]。激光光凝后注射 ATN-161 trifluoroacetate salt 可抑制脉络膜新生血管 (CNV) 渗漏和新生血管形成,其抑制程度与 AF564相似[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

711.67

Formula

C25H36F3N9O10S

CAS 号
性状

固体

颜色

White to off-white

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, 2 years; -20°C, 1 year (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O 中的溶解度 : 5 mg/mL (7.03 mM; 超声助溶 (<60°C))

DMSO 中的溶解度 : 1 mg/mL (1.41 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4051 mL 7.0257 mL 14.0515 mL
5 mM 0.2810 mL 1.4051 mL 2.8103 mL
查看完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 10 mg/mL (14.05 mM); 澄清溶液; 超声助溶 (<60°C)

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Cell Assay
[1]

Ninety-six well microtiter plates are coated with fibronectin(20 μg/mL) overnight at 4°C. 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 (1 μM) 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 200 μL) of the fibronectin-coated 96-well plates. Cells are incubated at 37°C 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 40 μL MTT to each well and incubating for 2 hr at 37°C. Media is then removed, cells are solubilized in 100 μL DMSO and optical density is measured at 560 nm. Experiments are performed in triplicate[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
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 50 μL 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 (100 mg/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, 50 mg/kg). On day 7, mice are anaesthetized again and osmotic pumps.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

ATN-161 trifluoroacetate salt 相关分类

完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 1.4051 mL 7.0257 mL 14.0515 mL 35.1286 mL
H2O 5 mM 0.2810 mL 1.4051 mL 2.8103 mL 7.0257 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
ATN-161 trifluoroacetate salt
目录号:
HY-13535A
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