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Cyclo(-RGDfK) TFA

カタログ番号GC60117

Cyclo(-RGDfK) TFA は、αvβ3 インテグリンの強力かつ選択的な阻害剤であり、IC50 は 0.94 nM です。 Cyclo(-RGDfK) TFA は、細胞表面の αvβ3 インテグリンへの特異的結合を介して、腫瘍微小血管系および癌細胞を強力に標的とします。

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Cyclo(-RGDfK) TFA 化学構造

Cas No.: 500577-51-5

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$203.00
在庫あり
5mg
$108.00
在庫あり
10mg
$167.00
在庫あり
50mg
$603.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description of Cyclo(-RGDfK) TFA

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].

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].

[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. [3]. V Lopez-Rodriguez, 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.

Chemical Properties of Cyclo(-RGDfK) TFA

Cas No. 500577-51-5 SDF
Canonical SMILES O=C(O)C(F)(F)F.O=C([C@H](CCCCN)NC([C@@H](CC1=CC=CC=C1)NC([C@H](CC(O)=O)NC(CN2)=O)=O)=O)N[C@@H](CCCNC(N)=N)C2=O
Formula C29H42F3N9O9 M.Wt 717.69
溶解度 DMSO: 100 mg/mL (139.34 mM); Water: 33.33 mg/mL (46.44 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Cyclo(-RGDfK) TFA

Prepare stock solution
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
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In vivo Formulation Calculator (Clear solution) of Cyclo(-RGDfK) TFA

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 1 reference(s) in Google Scholar.)

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