YHO-13177
Based on 2 publication(s) in Google Scholar
YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.65%
- CAS. Nr.: 912287-56-0
- Formel: C20H22N2O3S
- Molecular Weight:370.47
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Membrane Transporter/Ion Channel Compound Library
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Publications Citing Use of MedChemExpress (MCE) YHO-13177
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IF
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
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| HCT-116 | IC50 |
10 nM
Compound: 14; YHO-13177
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Cytotoxicity against human HCT-116 cells assessed as cell viability measured as mitochondrial NADH-dependent dehydrogenase activity incubated for 72 to 120 hrs
Cytotoxicity against human HCT-116 cells assessed as cell viability measured as mitochondrial NADH-dependent dehydrogenase activity incubated for 72 to 120 hrs
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[PMID: 37847948] |
YHO-13177 (0.01 to 1 μM, 96 h) reverses BCRP-mediated drug resistance and sensitivity in a concentration-dependent manner in various BCRP-transduced cancer cells[1].
YHO-13177 (0.01 to 1 μM, 96 h) decreases the expression of BCRP protein in HCT116 and HCT116/BCRP cells, or A549 and A549/SN4 cells[1].
YHO-13177 (0-0.1 μM, 96 h) reduces the side population cell ratio in HeLa cells in a concentration-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 and A549 cells
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Concentration:0.01 to 1 μM
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Incubation Time:96 h
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Result:Apparently decreased the level of BCRP protein at more than 24 hours.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCT116/BCRP xenograft mouse model[1]
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Dosage:19.7 μM or 27.3 μM
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Administration:19.7 μM, i.v., or 27.3 μM, p.o., a single dose for 25 days
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Result:Was maintained for at least 8 hours in plasma.
Chemical Information
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CAS. Nr. 912287-56-0
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Appearance Solid
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Molecular Weight 370.47
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Formel C20H22N2O3S
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Color Light yellow to yellow
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SMILES
N#C/C(C1=CC=C(OC)C(OC)=C1)=C\C2=CC=C(N3CCC(O)CC3)S2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Drug Deliv
2017 Nov;24(1):1453-1459. PMID: 28949254
YHO-13177 purchased from MedChemExpress. Usage Cited in: Drug Deliv. 2017 Nov;24(1):1453-1459. [Abstract]
Fluorescent substrates accumulate in the organoids. The organoids are incubated in Hoechst 33342 with or without YHO-13177 or Ko143 for 20, 60 and 100 minutes, respectively. Ko143 and YHO-13177 notably decrease the fluorescence intensity of Hoechst 33342 in the organoids.
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Crit Rev Anal Chem
A Critical Review on Advancement in Analytical Strategies for the Quantification of Clinically Relevant Biological Transporters. [Abstract]2022;52(7):1557-1571. PMID: 33691566
Lösungsmittel & Löslichkeit
DMSO : 33.33 mg/mL (89.97 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (6.75 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.
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.
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.
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Yamazaki R, et al. Novel acrylonitrile derivatives, YHO-13177 and YHO-13351, reverse BCRP/ABCG2-mediated drug resistance in vitro and in vivo. Mol Cancer Ther. 2011 Jul;10(7):1252-63. [Content Brief]
[2]. Shishido Y, et al. ABCG2 inhibitor YHO-13351 sensitizes cancer stem/initiating-like side population cells to irinotecan. Anticancer Res. 2013 Apr;33(4):1379-86. [Content Brief]
[3]. Yu S, et al. The mechanisms of multidrug resistance of breast cancer and research progress on related reversal agents. Bioorg Med Chem. 2023 Nov 15;95:117486. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.6993 mL | 13.4964 mL | 26.9927 mL | 67.4818 mL |
| 5 mM | 0.5399 mL | 2.6993 mL | 5.3985 mL | 13.4964 mL | |
| 10 mM | 0.2699 mL | 1.3496 mL | 2.6993 mL | 6.7482 mL | |
| 15 mM | 0.1800 mL | 0.8998 mL | 1.7995 mL | 4.4988 mL | |
| 20 mM | 0.1350 mL | 0.6748 mL | 1.3496 mL | 3.3741 mL | |
| 25 mM | 0.1080 mL | 0.5399 mL | 1.0797 mL | 2.6993 mL | |
| 30 mM | 0.0900 mL | 0.4499 mL | 0.8998 mL | 2.2494 mL | |
| 40 mM | 0.0675 mL | 0.3374 mL | 0.6748 mL | 1.6870 mL | |
| 50 mM | 0.0540 mL | 0.2699 mL | 0.5399 mL | 1.3496 mL | |
| 60 mM | 0.0450 mL | 0.2249 mL | 0.4499 mL | 1.1247 mL | |
| 80 mM | 0.0337 mL | 0.1687 mL | 0.3374 mL | 0.8435 mL |
YHO-13177 Related Classifications
HY-12757 Related Classifications
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