ErbB-2-binding peptide-1
Based on 1 Customer Validation
ErbB-2-binding peptide-1 (LTVSPWY) is a HER2 receptor-binding peptide. ErbB-2-binding peptide-1 can be conjugated with nuclear cross-linked micelles loaded with Doxorubicin (HY-15142A). ErbB-2-binding peptide-1 can also be radiolabeled to form 177Lu-DOTA-LTVSPWY. ErbB-2-binding peptide-1 is conjugated with antisense oligonucleotides. ErbB-2-binding peptide-1 can be used in research related to HER2-positive breast cancer and ovarian cancer.
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- Pureza : 99.52%
- No. CAS: 562791-56-4
- Fòrmula: C43H60N8O11
- Peso molecular:864.98
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Almacenamiento:
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
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HER2 |
RDC Peptide |
In Vitro
CCM conjugated with ErbB-2-binding peptide-1 shows significantly higher intracellular uptake in HER2-positive SKBR-3 cells compared with non-targeted or Herceptin-conjugated CCM, while it exhibits no selective uptake in HER2-negative MCF-10A cells[1].
ErbB-2-binding peptide-1 (30 min) inhibits the binding of Ph7-2 phage to SKBR3 breast cancer cells[2].
ErbB-2-binding peptide-1 binds to and internalizes into SKBR3 breast cancer cells, resulting in strong cytoplasmic staining[2].
ErbB-2-binding peptide-1 (1000-fold excess) effectively blocks the non-specific binding of 177Lu-DOTA-LTVSPWY to SKOV-3 cells, enabling accurate determination of the high affinity of this conjugate for the HER2 receptor, with a KD value of 6.6 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57 nude mice (female, 18-22 g)[3]
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Dosage:0.840 MBq (~1 µg) (biodistribution study); 15 MBq; 30 MBq
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Administration:i.v.
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Result:Showed tumor uptake of 0.92 %ID/g at 1 hour post-injection, 0.33 %ID/g at 4 hours post-injection, and 0.57 %ID/g at 48 hours post-injection.
Reached tumor-to-muscle ratios of 4.75 at 1 hour and 2.3 at 48 hours post-injection, while the tumor-to-blood ratio reached 13.97 at 48 hours post-injection.
Reduced tumor uptake by more than 2-fold at 4 hours post-injection after pre-injection of a 300-fold molar excess of non-labeled LTVSPWY.
Showed no significant difference in tumor growth between treatment and control groups over 21 days.
Resulted in a 62.5% mortality rate (5/8 mice) in the 30 MBq group, while the 15 MBq and control groups had a 37.5% mortality rate (3/8 mice each).
Induced cytoplasmic vacuolization in tumor tissue for both treatment groups, with more severe vacuolization in the 30 MBq group.
Caused epithelial cell separation from the glomerulus basement membrane and tubule lumen inflammation in kidney tissue, and inflated sinusoids, hemorrhage, and eosinophilic hepatocyte cytoplasm in liver tissue, with all tissue damage more severe in the 30 MBq group.
Chemical Information
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No. CAS 562791-56-4
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Appearance Solid
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Peso molecular 864.98
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Fòrmula C43H60N8O11
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Color White to off-white
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Synonyms
LTVSPWY
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Sequence
Leu-Thr-Val-Ser-Pro-Trp-Tyr
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Sequence Shortening
LTVSPWY
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (115.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.89 mM); 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 (2.89 mM); 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.
Protocolo
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Bayram NN, et al. HER2-Specific Peptide (LTVSPWY) and Antibody (Herceptin) Targeted Core Cross-Linked Micelles for Breast Cancer: A Comparative Study. Pharmaceutics. 2023 Feb 22;15(3):733. [Content Brief]
[2]. Shadidi M, et al. Identification of novel carrier peptides for the specific delivery of therapeutics into cancer cells. FASEB J. 2003 Feb;17(2):256-8. [Content Brief]
[3]. Molavipordanjani S, et al. The preclinical study of 177Lu-DOTA-LTVSPWY as a potential therapeutic agent against HER2 overexpressed cancer. Ann Nucl Med. 2023 Jul;37(7):400-409. [Content Brief]
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1561 mL | 5.7805 mL | 11.5610 mL | 28.9024 mL |
| 5 mM | 0.2312 mL | 1.1561 mL | 2.3122 mL | 5.7805 mL | |
| 10 mM | 0.1156 mL | 0.5780 mL | 1.1561 mL | 2.8902 mL | |
| 15 mM | 0.0771 mL | 0.3854 mL | 0.7707 mL | 1.9268 mL | |
| 20 mM | 0.0578 mL | 0.2890 mL | 0.5780 mL | 1.4451 mL | |
| 25 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1561 mL | |
| 30 mM | 0.0385 mL | 0.1927 mL | 0.3854 mL | 0.9634 mL | |
| 40 mM | 0.0289 mL | 0.1445 mL | 0.2890 mL | 0.7226 mL | |
| 50 mM | 0.0231 mL | 0.1156 mL | 0.2312 mL | 0.5780 mL | |
| 60 mM | 0.0193 mL | 0.0963 mL | 0.1927 mL | 0.4817 mL | |
| 80 mM | 0.0145 mL | 0.0723 mL | 0.1445 mL | 0.3613 mL | |
| 100 mM | 0.0116 mL | 0.0578 mL | 0.1156 mL | 0.2890 mL |
ErbB-2-binding peptide-1 Related Classifications
HY-P4082 Related Classifications
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