MAP855
Based on 1 Customer Validation
MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.37%
- No. CAS: 1660107-77-6
- Fòrmula: C28H23ClF2N6O3
- Peso molecular:564.97
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Actividad biológica
Descripciòn
IC50 & Target
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ERK 5 nM (EC50) |
MEK1 3 nM (IC50) |
In Vitro
MAP855 (compound 30) has single-digit nM inhibition of pERK and proliferation in A375 cells (pERK EC50=5 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A375 cells[1]
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Concentration:0-10 nM
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Incubation Time:72 hours
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Result:Showed single-digit nM inhibition of pERK and proliferation in A375 cells (pERK EC50=5 nM).
In Vivo
MAP855 (30 mg/kg; p.o., b.i.d, 14 days) achieves comparable efficacy to trametinib dosed at the mouse MTD without any body weight loss[1].
Pharmacokinetic Parameters of MAP855 in mouse, rat and dog[1].
| mouse | rat | dog | |
| CL [mL/min*kg] | 32 | 35 | 22 |
| Vss [l/kg] | 2.6 | 2.0 | 1.8 |
| AUC po d.n. [μM*h] | 0.4 | 0.6 | 1.4 |
| Oral BAV [% F] | 44 | 65 | 100 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar Rats[1]
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Dosage:3 mg/kg for i.v., 10 mg/kg for p.o.
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Administration:i.v. and p.o., single
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Result:Showed good oral bioavailability and medium clearance.
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Animal Model:A375 Tumor Bearing Mice[1]
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Dosage:30 mg/kg
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Administration:p.o., b.i.d, 14 days
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Result:Achieved comparable efficacy to trametinib dosed at the mouse MTD without any body weight loss.
Chemical Information
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No. CAS 1660107-77-6
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Appearance Solid
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Peso molecular 564.97
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Fòrmula C28H23ClF2N6O3
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Color Off-white to light yellow
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SMILES
CC1=NC2=C(C3=CC(C4=C(C=C(C=C4)OC5=NC=CC=N5)Cl)=C(F)C=C3N=C2)N1[C@]6([H])[C@H](CN(CC6)C(CO)=O)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 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (177.00 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. 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. 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 (4.43 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 (4.43 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.
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 (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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, 6 months; -20°C, 1 month. 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 | 1.7700 mL | 8.8500 mL | 17.7001 mL | 44.2501 mL |
| 5 mM | 0.3540 mL | 1.7700 mL | 3.5400 mL | 8.8500 mL | |
| 10 mM | 0.1770 mL | 0.8850 mL | 1.7700 mL | 4.4250 mL | |
| 15 mM | 0.1180 mL | 0.5900 mL | 1.1800 mL | 2.9500 mL | |
| 20 mM | 0.0885 mL | 0.4425 mL | 0.8850 mL | 2.2125 mL | |
| 25 mM | 0.0708 mL | 0.3540 mL | 0.7080 mL | 1.7700 mL | |
| 30 mM | 0.0590 mL | 0.2950 mL | 0.5900 mL | 1.4750 mL | |
| 40 mM | 0.0443 mL | 0.2213 mL | 0.4425 mL | 1.1063 mL | |
| 50 mM | 0.0354 mL | 0.1770 mL | 0.3540 mL | 0.8850 mL | |
| 60 mM | 0.0295 mL | 0.1475 mL | 0.2950 mL | 0.7375 mL | |
| 80 mM | 0.0221 mL | 0.1106 mL | 0.2213 mL | 0.5531 mL | |
| 100 mM | 0.0177 mL | 0.0885 mL | 0.1770 mL | 0.4425 mL |
MAP855 Related Classifications
HY-145702 Related Classifications
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