QPH-FR
Based on 1 Customer Validation
QPH-FR is a LGR5 inhibitor. QPH-FR competitively binds to LGR5 and prevents the formation of the LGR5/RSPO1 complex. QPH-FR promotes RNF43/ZNRF3-mediated ubiquitination of FZD receptors, inhibits the Wnt β-catenin signaling pathway, and reduces the stemness of colorectal cancer cells. QPH-FR is applicable to relevant research on colorectal cancer.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.54%
- 화학식: C81H124N26O25
- 분자량:1862.01
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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
QPH-FR binds to an overlapping site on LGR5 with RSPO1, with a binding energy of -7.0 kcal/mol, indicating potential competitive inhibition of LGR5/RSPO1 complex formation[1].
QPH-FR directly binds to endogenous LGR5 protein in HCT-8 and DLD1 human colorectal cancer cells[1].
QPH-FR (50 μg/mL; 24 h) enhances the chemosensitivity of HCT-8 and DLD1 human colorectal cancer cells to 5-FU, reducing the 5-FU IC50 to 11.27 μM and 15.30 μM, respectively[1].
QPH-FR (50 μg/mL; 24 h) inhibits tumor sphere formation, a marker of stemness, in HCT-8 and DLD1 human colorectal cancer cells by targeting LGR5, and blocks LiCl-induced Wnt pathway activation and sphere formation[1].
QPH-FR (20-60 μg/mL) disrupts the formation of the LGR5/RSPO1 complex in a dose-dependent manner in HCT-8 and DLD1 human colorectal cancer cells, with reduced RSPO1 binding to LGR5 at concentrations of 20, 40, and 60 μg/mL[1].
QPH-FR (50 μg/mL; 24 h) inhibits nuclear accumulation of β-catenin, a key mediator of Wnt signaling, in HCT-8 and DLD1 human colorectal cancer cells by targeting LGR5, and blocks LiCl-induced β-catenin nuclear translocation[1].
QPH-FR (50 μg/mL; 24 h) reduces the expression of stemness markers CD133, CD44, and ALDH1A1 at both the protein and mRNA levels in HCT-8 and DLD1 human colorectal cancer cells by targeting LGR5[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human colorectal cancer HCT-8 and DLD1 cells
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Concentration:50 μg/mL (co-incubated with 5-FU)
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Incubation Time:24 h (co-incubation with 5-FU)
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Result:Reduced the IC50 of 5-FU in HCT-8 cells from 49.57 μM to 11.27 μM.
Reduced the IC50 of 5-FU in DLD1 cells from 47.62 μM to 15.30 μM, indicating enhanced chemosensitivity of cells to 5-FU.
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Cell Line:Human colorectal cancer HCT-8 and DLD1 cells
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Concentration:50 μg/mL; 10 mM LiCl (co-incubated with QPH-FR)
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Incubation Time:24 h (QPH-FR treatment; QPH-FR + LiCl co-treatment)
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Result:Reduced nuclear β-catenin levels to near control levels when co-treated with LiCl, which alone increased total and nuclear β-catenin levels.
Lost inhibitory effect on nuclear β-catenin accumulation when LGR5 was knocked down.
Chemical Information
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Appearance Solid
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분자량 1862.01
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화학식 C81H124N26O25
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Color White to off-white
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Sequence
Phe-Lys-Glu-Asp-Val-Trp-Ser-Arg-Pro-Gly-Gly-Gly-Gly-Gly-Gly-Ile-Ser-Arg
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Sequence Shortening
FKEDVWSRPGGGGGGISR
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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 : 25 mg/mL (13.43 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 (1.34 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 (1.34 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
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.5371 mL | 2.6853 mL | 5.3705 mL | 13.4264 mL |
| 5 mM | 0.1074 mL | 0.5371 mL | 1.0741 mL | 2.6853 mL | |
| 10 mM | 0.0537 mL | 0.2685 mL | 0.5371 mL | 1.3426 mL |
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