2. Cytoskeleton
  3. Integrin
  4. Cyclo(-RGDfK) TFA

Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 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.

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Custom Peptide Synthesis

Cyclo(-RGDfK) TFA Chemical Structure

Cyclo(-RGDfK) TFA Chemical Structure

CAS No. : 500577-51-5

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5 mg USD 139 In-stock
10 mg USD 216 In-stock
25 mg USD 360 In-stock
50 mg USD 500 In-stock
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Based on 14 publication(s) in Google Scholar

Other Forms of Cyclo(-RGDfK) TFA:

Cyclo(-RGDfK) TFA Related Antibodies

Top Publications Citing Use of Products

View All Integrin Isoform Specific Products:

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 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

αvβ3

0.94 nM (IC50)

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].

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

Cyclo(-RGDfK) TFA Related Antibodies
Molecular Weight

717.69

Formula

C29H42F3N9O9
CAS No.
Appearance

Solid

Color

White to off-white

Sequence Shortening

Cyclo(RGDFK)
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
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)

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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.

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)

g

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: 99.82%

SDS (393 KB)

COA (255 KB) LCMS (258 KB)

Handling Instructions (2659 KB)
References

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.

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.

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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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