Cyclo(-RGDfK) TFA

Cyclo(-RGDfK) TFA; 纯度: 99.81%

Cyclo(-RGDfK) TFA 是有效,选择性的整合素 αvβ3 抑制剂,其 IC50 值为 0.94 nM。Cyclo(-RGDfK) TFA 通过与细胞表面的 αvβ3 整合素结合,特异性靶向肿瘤微血管和癌细胞。

Cyclo(-RGDfK) TFAamp;;

Cyclo(-RGDfK) TFA Chemical Structure

CAS No. : 500577-51-5

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ¥2190 In-stock
5 mg ¥1160 In-stock
10 mg ¥1800 In-stock
50 mg ¥6500 In-stock
100 mg ; 询价 ;
200 mg ; 询价 ;

* Please select Quantity before adding items.

Cyclo(-RGDfK) TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Macrocyclic Compound Library
  • Cytoskeleton Compound Library
  • Peptide Library

生物活性

Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM[1]. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface[3].

IC50 Target

IC50: 0.94 nM (αvβ3 integrin)[1]

体外研究
(In Vitro)

Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin and exhibits a IC50 of 0.94 nM[1].
[66Ga]DOTA-E-[c(RGDfK)]2 can be prepared with high radiochemical purity (>97%), specific activity (36-67GBq/μM), in vitro stability, and moderate protein binding. MicroPET imaging up to 24 post-injection showed contrasting tumors reflecting αvβ3-targeted tracer accumulation[2].

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

分子量

717.69

Formula

C29H42F3N9O9

CAS 号

500577-51-5

Sequence Shortening

Cyclo(RGDFK)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro:;

DMSO : 100 mg/mL (139.34 mM; Need ultrasonic)

H2O : 33.33 mg/mL (46.44 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3934 mL 6.9668 mL 13.9336 mL
5 mM 0.2787 mL 1.3934 mL 2.7867 mL
10 mM 0.1393 mL 0.6967 mL 1.3934 mL

*

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 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

  • 1.

    请依序添加每种溶剂:;PBS

    Solubility: 130 mg/mL (181.14 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂:;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.08 mg/mL (2.90 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.90 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂:;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (2.90 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.90 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂:;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.08 mg/mL (2.90 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.90 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • [1]. Simecek J, et al. Benefits of NOPO as chelator in gallium-68 peptides, exemplified by preclinical characterization of (68)Ga-NOPO-c(RGDfK). Mol Pharm. 2014 May 5;11(5):1687-95.

    [2]. Lopez-Rodriguez V, et al. Preparation and preclinical evaluation of (66)Ga-DOTA-E(c(RGDfK))2 as a potential theranostic radiopharmaceutical. Nucl Med Biol. 2015 Feb;42(2):109-14.