| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Cyclo(RADfK) targets the αvβ3 integrin, a cell surface receptor that plays a critical role in cell adhesion, migration, and angiogenesis. As a selective ligand for αvβ3 integrin, it binds to this receptor and modulates integrin-mediated signaling pathways. RGD peptides, including cyclo(RADfK), are recognized by various members of the integrin family and are modulators of cell adhesion.
|
|---|---|
| ln Vitro |
Cyclo(RADfK) is a negative control for cyclo(-RGDfK-) (RGD peptide). RGD peptides are modulators of cell adhesion and are recognized by various members of the integrin family [1].
In vitro, Cyclo(RADfK) binds selectively to αvβ3 integrin with high affinity. As a negative control for cyclo(-RGDfK-), it is used to distinguish specific integrin-mediated effects from non-specific effects in cell adhesion and angiogenesis assays. Its binding affinity and selectivity make it a valuable tool for studying integrin function. |
| ln Vivo |
In vivo, Cyclo(RADfK) is used in research, therapy, and diagnosis of neoangiogenesis. It is ideal for investigating tumor growth, angiogenic mechanisms, and potential therapeutic strategies targeting integrin-mediated interactions in various diseases. Its ability to bind selectively to αvβ3 integrin allows for targeted imaging and therapy of angiogenic tissues.
|
| Enzyme Assay |
In vitro receptor binding assays for Cyclo(RADfK) are conducted using cells expressing αvβ3 integrin. Radioligand binding assays with [¹²⁵I]-echistatin or fluorescently labeled RGD peptides are used to assess receptor binding affinity and specificity. Surface plasmon resonance (SPR) may also be used to measure real-time binding kinetics between the peptide and purified integrin.
|
| Cell Assay |
Cellular assays for Cyclo(RADfK) are performed using endothelial cells or cancer cell lines that express αvβ3 integrin. Cells are treated with the compound at concentrations ranging from 0.1 nM to 10 µM. Cell adhesion to integrin substrates (e.g., vitronectin, fibronectin) is assessed. Cell migration and invasion assays (Boyden chamber, wound healing) are also performed to evaluate the functional effects of integrin modulation.
|
| Animal Protocol |
In vivo animal studies for Cyclo(RADfK) are conducted in tumor xenograft models or models of angiogenesis. The compound is administered intravenously or intraperitoneally, often conjugated to imaging agents (e.g., fluorophores, radiotracers) or therapeutic payloads. Tumor growth, angiogenesis (measured by microvessel density), and biodistribution are assessed.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Cyclo(RADfK) are not well characterized. The compound has a molecular weight of 617.70 and a molecular formula of C₂₈H₄₃N₉O₇. As a cyclic peptide, it is expected to have moderate stability in vivo but may be susceptible to proteolytic degradation. Its half-life and bioavailability would depend on the route of administration and formulation.
|
| Toxicity/Toxicokinetics |
Toxicological data for Cyclo(RADfK) are limited. As a research peptide, it is designated for laboratory use only. No significant acute toxicity has been reported. Standard toxicity screening would be required for therapeutic development.
|
| References | |
| Additional Infomation |
Cyclo(RADfK) is a selective αvβ3 integrin ligand used for neoangiogenesis research, therapy, and diagnosis. It is a negative control for cyclo(-RGDfK-). It has a molecular weight of 617.70 and formula C₂₈H₄₃N₉O₇. It is not clinically approved.
|
| Molecular Formula |
C28H43N9O7
|
|---|---|
| Molecular Weight |
617.697125673294
|
| Exact Mass |
617.329
|
| CAS # |
756500-23-9
|
| PubChem CID |
45107783
|
| Appearance |
White to off-white solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Index of Refraction |
1.659
|
| LogP |
-2.75
|
| Hydrogen Bond Donor Count |
9
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
44
|
| Complexity |
1040
|
| Defined Atom Stereocenter Count |
5
|
| SMILES |
C[C@H]1C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CCCN=C(N)N)CCCCN)CC2=CC=CC=C2)CC(=O)O
|
| InChi Key |
SMFHXHGBDFBWOX-BWUHRYBWSA-N
|
| InChi Code |
InChI=1S/C28H43N9O7/c1-16-23(40)36-21(15-22(38)39)27(44)37-20(14-17-8-3-2-4-9-17)26(43)35-18(10-5-6-12-29)25(42)34-19(24(41)33-16)11-7-13-32-28(30)31/h2-4,8-9,16,18-21H,5-7,10-15,29H2,1H3,(H,33,41)(H,34,42)(H,35,43)(H,36,40)(H,37,44)(H,38,39)(H4,30,31,32)/t16-,18-,19-,20+,21-/m0/s1
|
| Chemical Name |
2-[(2S,5R,8S,11S,14S)-8-(4-aminobutyl)-5-benzyl-11-[3-(diaminomethylideneamino)propyl]-14-methyl-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : ~100 mg/mL (~161.89 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (161.89 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6189 mL | 8.0945 mL | 16.1891 mL | |
| 5 mM | 0.3238 mL | 1.6189 mL | 3.2378 mL | |
| 10 mM | 0.1619 mL | 0.8095 mL | 1.6189 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.