Peptide R54 acetate
Based on 1 Customer Validation
Peptide R54 acetate (Pep R54 acetate) is a CXCR4 antagonist. Peptide R54 acetate inhibits CXCL12-dependent activation of pERK1/2 and pAKT. The combination of Peptide R54 acetate and Nivolumab (HY-P9903) suppresses melanoma growth. Peptide R54 (acetate) is applicable to research related to melanoma and ovarian cancer.
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- Purity : 99.88%
- 화학식: C44H63N15O9S2·xC2H4O2
- 분자량:1010.20 (free base)
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보관:
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
CXCR4 |
CXCL12 |
ERK1 |
ERK2 |
In Vitro
Peptide R54 (100 nM; 16 h) acetate significantly inhibits CXCR4-dependent migration toward CXCL12 and CXCL11 in CAOV3, OVCAR8 and IGROV1 ovarian cancer cells[2].
Peptide R54 (100 nM; 24 h) acetate inhibits CXCR4-mediated mesenchymal transition by restoring the expression levels of EMT markers in CAOV3, OVCAR8 and IGROV1 ovarian cancer cells[2].
Peptide R54 (100 nM; 10 min) acetate inhibits CXCR4 downstream signaling pathways by reversing CXCL12-induced phosphorylation of ERK1/2, AKT and p38, as well as reversing the upregulation of RAC1 in CAOV3, OVCAR8 and IGROV1 ovarian cancer cells[2].
Peptide R54 (100 nM; 24-72 h) acetate attenuates CXCL12-induced proliferation and sensitizes CAOV3, OVCAR8 and IGROV1 ovarian cancer cells to cisplatin and paclitaxel[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human ovarian cancer CAOV3, OVCAR8, and IGROV1 cells
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Concentration:100 nM
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Incubation Time:16 h
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Result:Reduced the CXCL12-mediated migration index by 2.5-fold in CAOV3 (p<0.01), 2.1-fold in OVCAR8 (p<0.001), and 3-fold in IGROV1 (p<0.01) compared to CXCL12-only treatment.
Reduced the CXCL11-mediated migration index by 3-fold in IGROV1 (p<0.01) and 2-fold in OVCAR8 (p<0.001) compared to CXCL11-only treatment.
Had no impact on migration in CXCR4-knockout IGROV1 cells.
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Cell Line:human ovarian cancer CAOV3, OVCAR8, and IGROV1 cells
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Concentration:100 nM
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Incubation Time:10 min
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Result:Reversed CXCL12-induced phosphorylation of ERK1/2 and AKT in CAOV3 and OVCAR8; reversed only CXCL12-induced ERK1/2 phosphorylation in IGROV1.
Reversed CXCL12-induced p38 phosphorylation only in OVCAR8.
Reversed CXCL12-induced RAC1 upregulation mainly in IGROV1.
Had no effect on signaling proteins in CXCR4-knockout IGROV1 cells.
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Cell Line:human ovarian cancer CAOV3, OVCAR8, and IGROV1 cells
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Concentration:100 nM
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Incubation Time:24 h, 48 h, 72 h
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Result:Impaired CXCL12-induced proliferation in all three cell lines.
Reversed CXCL12-induced resistance to cisplatin and paclitaxel, potentiating the growth-inhibiting effects of the chemotherapeutic agents, particularly in OVCAR8 and IGROV1 treated with paclitaxel.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic Nude-Foxn1nu mice[1]
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Dosage:2 mg/kg
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Administration:i.p.; 5 days per week; 3 weeks
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Result:Reduced mean tumor volume to 410.33 mm3 compared to untreated controls (622.72 mm3) after 3 weeks of treatment (p = 0.038).
Reduced plasma lactate levels compared to untreated mice (Kruskal Wallis test P = 0.0209).
Showed a non-statistically significant reduction in lung disseminated PES43 tumor cells.
Decreased tumor CXCR4 and PD-L1 (mainly in stromal cells) expression.
Chemical Information
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Appearance Solid
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분자량 1010.20 (free base)
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화학식 C44H63N15O9S2·xC2H4O2
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Color White to off-white
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SMILES
O=C(N[C@@H](CCCNC(N)=N)C(N[C@@H](C)C(N[C@H](CSSC(C)([C@H](NC([C@@H](NC([C@@H](N1)CC(C=C2)=CC3=C2C=CC=C3)=O)CC4=CNC=N4)=O)C(O)=O)C)C(N[C@@H](CCCNC(N)=N)C1=O)=O)=O)=O)C.CC(O)=O.[x]
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Synonyms
Pep R54 acetate; CXCR4 antagonist peptide 19 acetate
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Sequence
Ac-Arg-Ala-cyclo{{d-Cys}-Arg-2-Nal-His-Pen}
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Sequence Shortening
Ac-RA-cyclo{{d-C}R-2-Nal-H-Pen}
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선적
Room temperature in continental US; may vary elsewhere.
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보관
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)
용액&용해도
In Vitro:
DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (284 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. D'Alterio C, et al. Targeting CXCR4 potentiates anti-PD-1 efficacy modifying the tumor microenvironment and inhibiting neoplastic PD-1. J Exp Clin Cancer Res. 2019;38(1):432. Published 2019 Oct 28. [Content Brief]
[2]. Russo D, et al. The CXCR4 antagonist R54 targets epithelial-mesenchymal transition (EMT) in human ovarian cancer cells. PLoS One. 2024;19(12):e0314735. Published 2024 Dec 19. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Peptide R54 acetate Related Classifications
HY-P11011A Related Classifications
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