Raf inhibitor 1
Based on 3 publication(s) in Google Scholar
Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively.
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- Pureza: 98.03%
- No. CAS: 1093100-40-3
- Fòrmula: C26H19ClN8
- Peso molecular:478.94
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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
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) Raf inhibitor 1
More
Actividad biológica
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B-Raf 1 nM (Ki) |
B-RafV600E 1 nM (Ki) |
C-Raf 0.3 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
0.002 μM
Compound: 13
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Inhibition of b-Raf in human A375 cells assessed phosphorylation of ERK
Inhibition of b-Raf in human A375 cells assessed phosphorylation of ERK
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[PMID: 22808911] |
| A-375 | IC50 |
0.31 μM
Compound: 13
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Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras
Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras
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[PMID: 22808911] |
| A-375 | IC50 |
2 nM
Compound: 1
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Inhibition of B-Raf V600E mutant in human A375 cells assessed as ERK phosphorylation preincubated for 1 hr by Western blot method
Inhibition of B-Raf V600E mutant in human A375 cells assessed as ERK phosphorylation preincubated for 1 hr by Western blot method
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[PMID: 27085672] |
| HCT-116 | IC50 |
0.72 μM
Compound: 13
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Antiproliferative activity against human HCT116 cells expressing wild type b-Raf and KRAS mutant
Antiproliferative activity against human HCT116 cells expressing wild type b-Raf and KRAS mutant
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[PMID: 22808911] |
| MIA PaCa-2 | EC50 |
22 nM
Compound: 1
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Inhibition of wild type B-Raf in human MIAPaCa2 cells assessed as reduction in ERK phosphorylation preincubated for 1 hr by Western blot method
Inhibition of wild type B-Raf in human MIAPaCa2 cells assessed as reduction in ERK phosphorylation preincubated for 1 hr by Western blot method
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[PMID: 27085672] |
Raf inhibitor 1 (Compound 13) inhibits A375 and HCT-116 proliferation with IC50s of 0.31 and 0.72 μM, respectively. Raf inhibitor 1 (Compound 13) binds to and stabilizes B-Raf in a DFG-out, inactive conformation in which the ATP pocket is partially filled by Phe595 and Gly596 from the DFG motif. Raf inhibitor 1 (Compound 13) additionally exhibits low micromolar inhibition against wild type B-Raf cell lines, which may be due to off-target kinase activities or alternatively to pan-Raf inhibition, including Raf dimers[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1093100-40-3
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Appearance Solid
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Peso molecular 478.94
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Fòrmula C26H19ClN8
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Color Light yellow to yellow
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SMILES
CC1=CC=C2C(C=CN=C2NC3=CC=C(Cl)C=C3)=C1NC4=NC=CC=C4C5=NC=NC6=C5N=CN6
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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 (3)
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Journal Impact Factor
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Most Recent
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J Med Chem
Conformational analysis of the DFG-out kinase motif and biochemical profiling of structurally validated type II inhibitors. [Abstract]2015 Jan 8;58(1):466-79. PMID: 25478866 -
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Solvente y solubilidad
DMSO : 50 mg/mL (104.40 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)
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 (5.22 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 (5.22 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 (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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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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0879 mL | 10.4397 mL | 20.8794 mL | 52.1986 mL |
| 5 mM | 0.4176 mL | 2.0879 mL | 4.1759 mL | 10.4397 mL | |
| 10 mM | 0.2088 mL | 1.0440 mL | 2.0879 mL | 5.2199 mL | |
| 15 mM | 0.1392 mL | 0.6960 mL | 1.3920 mL | 3.4799 mL | |
| 20 mM | 0.1044 mL | 0.5220 mL | 1.0440 mL | 2.6099 mL | |
| 25 mM | 0.0835 mL | 0.4176 mL | 0.8352 mL | 2.0879 mL | |
| 30 mM | 0.0696 mL | 0.3480 mL | 0.6960 mL | 1.7400 mL | |
| 40 mM | 0.0522 mL | 0.2610 mL | 0.5220 mL | 1.3050 mL | |
| 50 mM | 0.0418 mL | 0.2088 mL | 0.4176 mL | 1.0440 mL | |
| 60 mM | 0.0348 mL | 0.1740 mL | 0.3480 mL | 0.8700 mL | |
| 80 mM | 0.0261 mL | 0.1305 mL | 0.2610 mL | 0.6525 mL | |
| 100 mM | 0.0209 mL | 0.1044 mL | 0.2088 mL | 0.5220 mL |
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