MK-4101
Based on 1 Customer Validation
MK-4101 is a Smoothened (SMO) antagonist (IC50 of 1.1 µM for 293 cells ) and also a potent inhibitor of the hedgehog pathway (IC50 of 1.5 µM for mouse cells; IC50 of 1 µM for KYSE180 oesophageal cancer cells). MK-4101 has robust antitumor activity that inhibits tumor cell proliferation and induces extensive apoptosis.
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- Pureza: 99.16%
- No. CAS: 935273-79-3
- Fòrmula: C24H24F5N5O
- Peso molecular:493.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
- Pureza y Documentación
- Referencias
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Stem Cell Signaling Compound Library
HY-L017
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Wnt/Hedgehog/Notch Compound Library
HY-L020
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Differentiation Inducing Compound Library
HY-L038
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Pancreatic Cancer Compound Library
HY-L077
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Anti-Blood Cancer Compound Library
HY-L079
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Anti-Liver Cancer Compound Library
HY-L101
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Anti-Colorectal Cancer Compound Library
HY-L103
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Cancer Stem Cells Compound Library
HY-L135
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Cell Death Library
HY-L162
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Anti-Hematopathy Compound Library
HY-L171
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Anti-Gastric Cancer Compound Library
HY-L184
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Anti-Fibrosis Compound Library
HY-L185
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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Cell Proliferation Compound Library
HY-L201
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High-Throughput Bioactive Compound Library
HY-L205
Actividad biológica
IC50: 1.1 µM (293 cells ); 1.5 µM (mouse cells); 1 µM (KYSE180 oesophageal cancer cells)[1]
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Cell Line
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Type | Value | Description | References |
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| Medulloblastoma cell | IC50 |
0.3 μM
Compound: MK-4101
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Antiproliferative activity against neonatally irradiated Ptch1-/+ mouse medulloblastoma cells assessed as inhibition of cell proliferation
Antiproliferative activity against neonatally irradiated Ptch1-/+ mouse medulloblastoma cells assessed as inhibition of cell proliferation
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[PMID: 33636537] |
MK-4101 inhibits Hh signaling both in a reporter gene assay in an engineered mouse cell line with an IC50 of 1.5 µM, and in human KYSE180 oesophageal cancer cells with an IC50 of 1 µM. MK-4101 displaces a fluorescently-labeled cyclopamine derivative from 293 cells expressing recombinant human SMO with an IC50 of 1.1 µM, implying that the compound binds to SMO. MK4101 also inhibits the proliferation of medulloblastoma cells derived from neonatallyirradiated Ptch1-/+ mice in vitro with an IC50 of 0.3 µM[1].
MK-4101 (10 µM; 60 hours, 72 hours; medulloblastoma or BCC cells) treatment shows cell cycle arrest with a nearly complete disappearance of the S phase subpopulation, a prominent increase of the G1 population and, to a minor extent, of the G2 population[1].
MK-4101 (10 µM; medulloblastoma or BCC cells) treatment significantly reduces cyclin D1 protein and accumulation of cyclin B1 protein[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Medulloblastoma or BCC cells
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Concentration:10 µM
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Incubation Time:60 hours, 72 hours
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Result:Showed cell cycle arrest.
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Cell Line:Medulloblastoma or BCC cells
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Concentration:10 µM
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Incubation Time:
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Result:Significant reduction of cyclin D1 protein and accumulation of cyclin B1 protein.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5-weeks old CD1 nude female mice with medulloblastoma/BCC cells[1]
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Dosage:40 or 80 mg/kg once a day, 80 mg/kg twice a day
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Administration:Oral administration; for 3.5 weeks
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Result:Showed tumor growth inhibition (40 and 80 mg/kg ) and tumor regression at the highest dose (80 mg/kg).
Chemical Information
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No. CAS 935273-79-3
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Appearance Solid
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Peso molecular 493.47
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Fòrmula C24H24F5N5O
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Color White to off-white
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SMILES
FC(C1=CC=CC=C1C2=NN=C(C34CCC(C5=NOC(C6CC(F)(F)C6)=N5)(CC4)CC3)N2C)(F)F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : ≥ 50 mg/mL (101.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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 (5.07 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 (5.07 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.
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.
Pureza y Documentación
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Ficha de datos (276 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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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.0265 mL | 10.1323 mL | 20.2647 mL | 50.6616 mL |
| 5 mM | 0.4053 mL | 2.0265 mL | 4.0529 mL | 10.1323 mL | |
| 10 mM | 0.2026 mL | 1.0132 mL | 2.0265 mL | 5.0662 mL | |
| 15 mM | 0.1351 mL | 0.6755 mL | 1.3510 mL | 3.3774 mL | |
| 20 mM | 0.1013 mL | 0.5066 mL | 1.0132 mL | 2.5331 mL | |
| 25 mM | 0.0811 mL | 0.4053 mL | 0.8106 mL | 2.0265 mL | |
| 30 mM | 0.0675 mL | 0.3377 mL | 0.6755 mL | 1.6887 mL | |
| 40 mM | 0.0507 mL | 0.2533 mL | 0.5066 mL | 1.2665 mL | |
| 50 mM | 0.0405 mL | 0.2026 mL | 0.4053 mL | 1.0132 mL | |
| 60 mM | 0.0338 mL | 0.1689 mL | 0.3377 mL | 0.8444 mL | |
| 80 mM | 0.0253 mL | 0.1267 mL | 0.2533 mL | 0.6333 mL | |
| 100 mM | 0.0203 mL | 0.1013 mL | 0.2026 mL | 0.5066 mL |
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