Pep-20
Based on 1 Customer Validation
Pep-20 is a CD47 binder with a human Kd of 2.91 µM and a murine Kd of 3.63 µM. Pep-20 blocks the interaction between CD47 and SIRPα, with an IC50 of 24.56 µM for human targets and 12.03 µM for murine targets. Pep-20 also acts as a phagocytosis enhancer and an inducer of anti-tumor immune responses. By blocking the CD47/SIRPα interaction, Pep-20 reduces the tyrosine phosphorylation level of SIRPα, disrupts the inhibitory "don't eat me" signaling pathway, enhances macrophage-mediated phagocytosis of solid tumor cells and hematologic tumor cells, and promotes macrophage mobilization of anti-tumor T-cell responses. Pep-20 can be used in research related to solid tumors, hematologic malignancies, breast cancer, and pancreatic cancer.
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- Purity: 99.94%
- CAS No.: 3056822-31-9
- 화학식: C74H93N21O18
- 분자량:1564.66
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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
Pep-20 (30 min) binds to purified human CD47-IgV-Domain protein with a KD of 2.91 µM[1].
Pep-20 (30 min) binds to purified mouse CD47-IgV-Domain protein with a KD of 3.63 µM[1].
Pep-20 (30 min-1 h) blocks the interaction between human CD47 and SIRPα with an IC50 of 24.56 µM[1].
Pep-20 (30 min-1 h) blocks the interaction between mouse CD47 and SIRPα with an IC50 of ~12.03 µM[1].
Pep-20 (100 µM; 4 h) significantly enhances human peripheral blood-derived macrophage-mediated phagocytosis of GFP+ MCF7 human breast cancer cells in vitro[1].
Pep-20 (100 µM; 4 h) significantly enhances human peripheral blood-derived macrophage-mediated phagocytosis of GFP+ HT29 human colorectal cancer cells in vitro[1].
Pep-20 (100 µM; 4 h) significantly enhances human peripheral blood-derived macrophage-mediated phagocytosis of GFP+ Jurkat human acute T cell leukemia cells in vitro[1].
Pep-20 (100 µM; 4 h) significantly enhances mouse bone marrow-derived macrophage-mediated phagocytosis of CFSE+ CT26 mouse colorectal cancer cells in vitro[1].
Pep-20 (100 µM; 4 h) significantly enhances mouse bone marrow-derived macrophage-mediated phagocytosis of GFP+ MC38 mouse colorectal cancer cells in vitro[1].
Pep-20 (100 µM; 4 h) significantly enhances mouse bone marrow-derived macrophage-mediated phagocytosis of GFP+ B16-OVA mouse melanoma cells in vitro[1].
Pep-20 reduces SIRPα tyrosine phosphorylation in mouse bone marrow-derived macrophages co-cultured with CT26 mouse colorectal cancer cells, confirming direct CD47/SIRPα interaction blockade[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Cmax |
|---|---|---|---|---|
| Mice[1] | 40 mg/kg | i.v. | 0.59 h | 33.60 ng/mL |
Pep-20 (2 mg/kg; s.c., peritumoral; daily; 14 days) delays CT26 tumor growth in BALB/c mice, prolongs overall survival, and activates antitumor CD8+ T-cell immune responses[1].
Pep-20 (2 mg/kg; s.c., peritumoral; daily; 14 days) significantly suppresses B16-OVA melanoma growth in C57BL/6 mice and activates antigen-specific antitumor CD8+ T-cell immune responses[1].
Pep-20 (2 mg/kg; s.c., peritumoral; daily; 14 days) has antitumor efficacy and CD8+ T-cell activating effects in MC38 tumor-bearing C57BL/6 mice that are dependent on macrophages[1].
Pep-20 (2 mg/kg; s.c.; daily; 14 days) does not induce significant toxicity, including anemia, in naïve C57BL/6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (subcutaneously injected with 1×106 MC38 cells)[1]
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Dosage:2 mg/kg
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Administration:s.c., peritumoral; daily; 14 days
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Result:Significantly suppressed tumor growth.
Prolonged overall survival (log-rank P=0.044, HR=2.642).
Increased intratumoral CD8+ T cells from 11.1% to 33.7% of total CD45+ cells.
Increased IFN-γ-expressing CD8+ T cells from 14.2% to 22.7% in draining lymph nodes and from 15% to 22.5% in spleens.
Increased IFN-γ secretion in draining lymph node supernatants to ~3 ng/mL (from ~1 ng/mL in controls).
Increased IFN-γ secretion in spleen supernatants to ~80 ng/mL (from ~20 ng/mL in controls).
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Animal Model:BALB/c (subcutaneously injected with 2×105 CT26 cells)[1]
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Dosage:2 mg/kg
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Administration:s.c., peritumoral; daily; 14 days
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Result:Delayed tumor growth.
Prolonged overall survival compared to normal saline controls.
Increased intratumoral CD8+ T-cell populations.
Boosted frequencies of IFN-γ-expressing CD8+ T cells in draining lymph nodes and spleens.
Elevated IFN-γ secretion in cellular supernatants from draining lymph nodes and spleens.
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Animal Model:C57BL/6 (subcutaneously injected with 2×105 B16-OVA cells)[1]
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Dosage:2 mg/kg
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Administration:s.c., peritumoral; daily; 14 days
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Result:Significantly suppressed tumor growth.
Increased intratumoral CD8+ T cells from 6.1% to 11.4% of total CD45+ cells.
Increased IFN-γ-expressing CD8+ T cells from 0.07% to 0.3% in draining lymph nodes and from 0.35% to 0.54% in spleens after OVA257-264 peptide stimulation.
Increased IFN-γ secretion in draining lymph node supernatants to ~1.5 ng/mL (from ~0.1 ng/mL in controls).
Increased IFN-γ secretion in spleen supernatants to ~2 ng/mL (from ~0.5 ng/mL in controls).
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Animal Model:C57BL/6 (subcutaneously injected with 1×106 MC38 cells; macrophage depletion via clodronate liposomes)[1]
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Dosage:2 mg/kg
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Administration:s.c., peritumoral; daily; 14 days
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Result:Significantly suppressed tumor growth in mice receiving control liposomes compared to normal saline controls.
Showed no significant tumor growth difference in macrophage-depleted mice compared to normal saline controls.
Increased intratumoral CD8+ T cells from 0.64% to 8.83% of total CD45+ cells in control liposome-treated mice; this increase was attenuated in macrophage-depleted mice (pep-20 group reached 6.73%, compared to 1.93% in saline controls).
Increased IFN-γ-expressing CD8+ T cells from 19.4% to 28.8% in draining lymph nodes and from 14.4% to 26.6% in spleens of control liposome-treated mice.
Showed no significant difference in frequencies of IFN-γ-expressing CD8+ T cells between pep-20 and normal saline groups in macrophage-depleted mice.
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Animal Model:C57BL/6 (naïve)[1]
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Dosage:2 mg/kg
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Administration:s.c.; daily; 14 days
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Result:Caused no significant differences in red blood cell count, hemoglobin level, organ coefficients, or hepatic damage markers compared to pre-treatment or control values.
Showed no abnormalities in histopathology analysis of major organs.
Chemical Information
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CAS No. 3056822-31-9
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Appearance Solid
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분자량 1564.66
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화학식 C74H93N21O18
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Color White to off-white
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Sequence
Ala-Trp-Ser-Ala-Thr-Trp-Ser-Asn-Tyr-Trp-Arg-His
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Sequence Shortening
AWSATWSNYWRH
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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
DMSO : 100 mg/mL (63.91 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)
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 (1.60 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 (1.60 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.
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
References
[1]. Wang H, et al. CD47/SIRPα blocking peptide identification and synergistic effect with irradiation for cancer immunotherapy. Journal for immunotherapy of cancer. 2020 Oct;8(2):e000905. [Content Brief]
[2]. Zhang W, et al. An in-situ peptide-antibody self-assembly to block CD47 and CD24 signaling enhances macrophage-mediated phagocytosis and anti-tumor immune responses. Nature communications. 2024 Jul 06;15(1):5670. [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 |
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| DMSO | 1 mM | 0.6391 mL | 3.1956 mL | 6.3912 mL | 15.9779 mL |
| 5 mM | 0.1278 mL | 0.6391 mL | 1.2782 mL | 3.1956 mL | |
| 10 mM | 0.0639 mL | 0.3196 mL | 0.6391 mL | 1.5978 mL | |
| 15 mM | 0.0426 mL | 0.2130 mL | 0.4261 mL | 1.0652 mL | |
| 20 mM | 0.0320 mL | 0.1598 mL | 0.3196 mL | 0.7989 mL | |
| 25 mM | 0.0256 mL | 0.1278 mL | 0.2556 mL | 0.6391 mL | |
| 30 mM | 0.0213 mL | 0.1065 mL | 0.2130 mL | 0.5326 mL | |
| 40 mM | 0.0160 mL | 0.0799 mL | 0.1598 mL | 0.3994 mL | |
| 50 mM | 0.0128 mL | 0.0639 mL | 0.1278 mL | 0.3196 mL | |
| 60 mM | 0.0107 mL | 0.0533 mL | 0.1065 mL | 0.2663 mL |
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