RO4987655
Based on 6 publication(s) in Google Scholar
RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM for inhibition of MEK1/MEK2.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.01%
- No. CAS: 874101-00-5
- Fòrmula: C20H19F3IN3O5
- Peso molecular:565.28
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) RO4987655
MoreVer todos los productos específicos de isoformas MEK
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
MEK1 5.2 nM (IC50) |
MEK2 5.2 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C32 | IC50 |
8.4 nM
Compound: 24, CH4987655
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Cytotoxicity against human C32 cells expressing b-Raf V600E mutant after 4 days
Cytotoxicity against human C32 cells expressing b-Raf V600E mutant after 4 days
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[PMID: 21316218] |
| COLO 205 | IC50 |
0.86 nM
Compound: 24, CH4987655
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Cytotoxicity against human COLO205 cells expressing b-Raf V600E mutant after 4 days
Cytotoxicity against human COLO205 cells expressing b-Raf V600E mutant after 4 days
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[PMID: 21316218] |
| HT-29 | IC50 |
1.7 nM
Compound: 24, CH4987655
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Cytotoxicity against human HT-29 cells expressing b-Raf V600E mutant after 4 days
Cytotoxicity against human HT-29 cells expressing b-Raf V600E mutant after 4 days
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[PMID: 21316218] |
| MIA PaCa-2 | IC50 |
3.3 nM
Compound: 24, CH4987655
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Cytotoxicity against human MIAPaCa2 cells expressing Kras G12C mutant after 4 days
Cytotoxicity against human MIAPaCa2 cells expressing Kras G12C mutant after 4 days
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[PMID: 21316218] |
| QG-56 | IC50 |
9.5 nM
Compound: 24, CH4987655
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Cytotoxicity against human QG56 cells expressing Hras Q61L mutant after 4 days
Cytotoxicity against human QG56 cells expressing Hras Q61L mutant after 4 days
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[PMID: 21316218] |
In Vitro
RO4987655 potently inhibits mitogen-activated protein kinase signaling pathway activation and tumor cell growth, with an in vitro IC50 of 5.2 nM for inhibition of MEK1/2[1]. RO4987655 inhibits proliferation of NCI-H2122 cells in a dose-dependent manner with an IC50 value of 0.0065 μM. RO4987655 at doses ranging from 0.1 to 1.0 μM suppresses pERK1/2 already at 2 h after the start of treatment[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 874101-00-5
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Appearance Solid
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Peso molecular 565.28
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Fòrmula C20H19F3IN3O5
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Color White to off-white
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SMILES
FC(C(F)=C(NC1=CC=C(I)C=C1F)C(C(NOCCO)=O)=C2)=C2CN3C(CCCO3)=O
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Synonyms
CH4987655
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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
Publications (6)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Cancer Discov
Exploiting Allosteric Properties of RAF and MEK Inhibitors to Target Therapy-Resistant Tumors Driven by Oncogenic BRAF Signaling. [Abstract]2021 Jul;11(7):1716-1735. PMID: 33568355 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
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ACS Comb Sci
Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]2019 Dec 9;21(12):805-816. PMID: 31689077
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (176.90 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.
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 (4.42 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 (4.42 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.
Protocolo
Cell Assay[2]
The human lung adenocarcinoma cell line NCI-H2122 are maintained in the designated media and indicated concentrations of heat-inactivated fetal bovine serum and L-glutamine. Cells are grown at 37°C in an atmosphere of 5%CO2. Cells are treated with various concentrations of RO4987655 (0.00001, 0.001, 0.1, and 10 μM) for 72 h in 96-well plates and viable cells were quantified with Cell Counting Kit-8[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[2]
Mice[2]
Female athymic nude mice Balb nu/nu, age 5 to 6 weeks (18 to 22 g) are used. NCI-H2122 cells (4×106/mouse) are inoculated subcutaneously in the right flank of Balb-nu/nu mice. Once tumors are established (100 to 200 mm3), mice are randomized into groups with similar mean tumor volumes at the start of the study. The tumors size is estimated with digital caliper and PET scans performed on days 0, 1, and 3 with 1.0, 2.5, and 5.0 mg/kg RO4987655. Tumor volume and body weight are measured on days 0 (baseline), 1, 2, 3, and 9 of [18F] FDG-PET imaging. Tumor growth inhibition is calculated[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Lee L, et al. The safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of CH4987655 in healthy volunteers: target suppression using a biomarker. Clin Cancer Res. 2009 Dec 1;15(23):7368-74. [Content Brief]
[2]. Tegnebratt T, et al. Evaluation of efficacy of a new MEK inhibitor, RO4987655, in human tumor xenografts by [(18)F] FDG-PET imaging combined with proteomic approaches. EJNMMI Res. 2014 Dec;4(1):34. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7690 mL | 8.8452 mL | 17.6903 mL | 44.2259 mL |
| 5 mM | 0.3538 mL | 1.7690 mL | 3.5381 mL | 8.8452 mL | |
| 10 mM | 0.1769 mL | 0.8845 mL | 1.7690 mL | 4.4226 mL | |
| 15 mM | 0.1179 mL | 0.5897 mL | 1.1794 mL | 2.9484 mL | |
| 20 mM | 0.0885 mL | 0.4423 mL | 0.8845 mL | 2.2113 mL | |
| 25 mM | 0.0708 mL | 0.3538 mL | 0.7076 mL | 1.7690 mL | |
| 30 mM | 0.0590 mL | 0.2948 mL | 0.5897 mL | 1.4742 mL | |
| 40 mM | 0.0442 mL | 0.2211 mL | 0.4423 mL | 1.1056 mL | |
| 50 mM | 0.0354 mL | 0.1769 mL | 0.3538 mL | 0.8845 mL | |
| 60 mM | 0.0295 mL | 0.1474 mL | 0.2948 mL | 0.7371 mL | |
| 80 mM | 0.0221 mL | 0.1106 mL | 0.2211 mL | 0.5528 mL | |
| 100 mM | 0.0177 mL | 0.0885 mL | 0.1769 mL | 0.4423 mL |
RO4987655 Related Classifications
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