Cyclo(-RGDfK) TFA

Name: Cyclo(-RGDfK) TFA
Brand: MedChemExpress
SKU: HY-P0023A
Rating: 5.0 (27 reviews)

Cat. No.: HY-P0023A Purity: 99.61%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the α_vβ₃ integrin, with an IC₅₀ of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

CAS No. : 500577-51-5

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 27 publication(s) in Google Scholar

Other Forms of Cyclo(-RGDfK) TFA:

Cyclo(-RGDfK) In-stock

27 Publications Citing Use of MCE Cyclo(-RGDfK) TFA

Bio/Physico-chemical Assay

Cell Migration/Invasion Assay

Cell Proliferation/Viability Assay

In Vivo Efficacy Study

: Cyclo(-RGDfK) TFA purchased from MedChemExpress. Usage Cited in: Mater Today. 2026 Jan 7;92:453-472.; Cyclo(-RGDfK) (200 μM; 1 h; 37 ℃) significantly reduced intracellular fluorescence intensity, indicating that the constructed LNP-RGD nanoparticles achieved efficient and targeted cellular uptake through RGD–integrin αvβ3 interactions.

: Cyclo(-RGDfK) TFA purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2025 Aug;14(8):e70146. [Abstract]; Integrin αVβ3 inhibitor Cyclo(-RGDfK) (10 μM) pretreatment prevented the S-EMs-induced proliferation of WKY and SHR 24 h after the application of the S-EMs.

: Cyclo(-RGDfK) TFA purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2025 Aug;14(8):e70146. [Abstract]; Integrin αVβ3 inhibitor Cyclo(-RGDfK) (10 μM) prevented the increased ratios of P-PI3K/PI3K, P-AKT/AKT, and P-FAK/FAK in VSMCs of WKY and SHR that were promoted by S-EMs.

: Cyclo(-RGDfK) TFA purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2025 Aug;14(8):e70146. [Abstract]; Cyclo (-RGDfK) (10 mg/kg; i.p.; every 2 d for 10 times) almost abolished vascular remodelling induced by S-EMs in the aorta of WKY mice.

: Cyclo(-RGDfK) TFA purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2021 Jan 7;6(7):2039-2057. [Abstract]; The integrin αvβ3 inhibitor Cyclo(-RGDfK) (20 μM; 1 h) significantly inhibited MSC migration.

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View All Isoforms

αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

Biological Activity
Purity & Documentation
References
Customer Review

Description

Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the α_vβ₃ 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

αvβ3

0.94 nM (IC₅₀)

In Vitro

Cyclo(-RGDfK) is a potent and selective inhibitor of the α_vβ₃ 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 α_vβ₃-targeted tracer accumulation^[2].

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

Molecular Weight

717.69

Formula

C₂₉H₄₂F₃N₉O₉

CAS No.

500577-51-5

Appearance

Solid

Color

White to off-white

Sequence

Cyclo(Arg-Gly-Asp-{dPhe}-Lys)

Sequence Shortening

Cyclo(RGD-{dPhe}-K)

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (139.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (2.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (2.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (2.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 130 mg/mL (181.14 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.61%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (254 KB) RP-HPLC (262 KB) MS (70 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.3934 mL	6.9668 mL	13.9336 mL	34.8340 mL
	5 mM	0.2787 mL	1.3934 mL	2.7867 mL	6.9668 mL
	10 mM	0.1393 mL	0.6967 mL	1.3934 mL	3.4834 mL
	15 mM	0.0929 mL	0.4645 mL	0.9289 mL	2.3223 mL
	20 mM	0.0697 mL	0.3483 mL	0.6967 mL	1.7417 mL
	25 mM	0.0557 mL	0.2787 mL	0.5573 mL	1.3934 mL
	30 mM	0.0464 mL	0.2322 mL	0.4645 mL	1.1611 mL
	40 mM	0.0348 mL	0.1742 mL	0.3483 mL	0.8708 mL
DMSO	50 mM	0.0279 mL	0.1393 mL	0.2787 mL	0.6967 mL
	60 mM	0.0232 mL	0.1161 mL	0.2322 mL	0.5806 mL
	80 mM	0.0174 mL	0.0871 mL	0.1742 mL	0.4354 mL
	100 mM	0.0139 mL	0.0697 mL	0.1393 mL	0.3483 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Cyclo(-RGDfK) TFA Related Classifications

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.

Keywords:

Cyclo(-RGDfK)500577-51-5IntegrinMicrovasculaturecancerαvβ3 integrintumoral cellligandInhibitorinhibitorinhibit

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Cyclo(-RGDfK) TFA

Customer Review

Other Forms of Cyclo(-RGDfK) TFA:

Cyclo(-RGDfK) TFA Related Antibodies

27 Publications Citing Use of MCE Cyclo(-RGDfK) TFA

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Integrin Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Cyclo(-RGDfK) TFA Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Cyclo(-RGDfK) TFA Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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