MAPK-IN-2
Based on 1 Customer Validation
MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFRWT IC50=281 nM, c-MET IC50=205 nM, B-RAFWT IC50=112 nM, and CDK4/6 IC50=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFRT790M IC50=69 nM and B-RAFV600E IC50=83 nM).
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- Pureza: 99.66%
- No. CAS: 3052814-46-4
- Fòrmula: C20H11Cl2N3O
- Peso molecular:380.23
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
IC50: 281 nM (EGFRWT), 69 nM (EGFRT790M), 205 nM (c-MET), 112 nM (B-RAFWT), 83 nM (B-RAFV600E), 95 nM (CDK4), 184 nM (CDK6)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| FHC | GI50 |
26.84 μM
Compound: 3h
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Cytotoxicity against human FHC cells assessed as cell growth inhibition incubated for 4 days by MTT assay
Cytotoxicity against human FHC cells assessed as cell growth inhibition incubated for 4 days by MTT assay
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[PMID: 37506545] |
| HCT-116 | GI50 |
2.53 μM
Compound: 3h
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Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition incubated for 4 days by MTT assay
Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition incubated for 4 days by MTT assay
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[PMID: 37506545] |
| HEK293 | GI50 |
22.4 μM
Compound: 3h
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Cytotoxicity against human HEK293 cells assessed as cell growth inhibition incubated for 4 days by MTT assay
Cytotoxicity against human HEK293 cells assessed as cell growth inhibition incubated for 4 days by MTT assay
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[PMID: 37506545] |
| HOP-92 | GI50 |
0.75 μM
Compound: 3h
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Cytotoxicity against human HOP-92 cells assessed as cell growth inhibition incubated for 4 days by MTT assay
Cytotoxicity against human HOP-92 cells assessed as cell growth inhibition incubated for 4 days by MTT assay
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[PMID: 37506545] |
| MRC5 | GI50 |
28.48 μM
Compound: 3h
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Cytotoxicity against human MRC5 cells assessed as cell growth inhibition incubated for 4 days by MTT assay
Cytotoxicity against human MRC5 cells assessed as cell growth inhibition incubated for 4 days by MTT assay
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[PMID: 37506545] |
| RXF 393 | GI50 |
3.12 μM
Compound: 3h
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Cytotoxicity against human RXF 393 cells assessed as cell growth inhibition incubated for 4 days by MTT assay
Cytotoxicity against human RXF 393 cells assessed as cell growth inhibition incubated for 4 days by MTT assay
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[PMID: 37506545] |
| SR | GI50 |
2.77 μM
Compound: 3h
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Cytotoxicity against human SR cells assessed as cell growth inhibition incubated for 4 days by MTT assay
Cytotoxicity against human SR cells assessed as cell growth inhibition incubated for 4 days by MTT assay
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[PMID: 37506545] |
Chemical Information
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No. CAS 3052814-46-4
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Appearance Solid
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Peso molecular 380.23
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Fòrmula C20H11Cl2N3O
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Color Light yellow to orange
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SMILES
O=C1C(C#N)=C(C2=CC=C(Cl)C=C2Cl)C=C(C3=CNC4=C3C=CC=C4)N1
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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
DMSO : 16.67 mg/mL (43.84 mM; ultrasonic and warming and heat to 60°C; 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)
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: 1.67 mg/mL (4.39 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.67 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 (16.7 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.
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6300 mL | 13.1499 mL | 26.2999 mL | 65.7497 mL |
| 5 mM | 0.5260 mL | 2.6300 mL | 5.2600 mL | 13.1499 mL | |
| 10 mM | 0.2630 mL | 1.3150 mL | 2.6300 mL | 6.5750 mL | |
| 15 mM | 0.1753 mL | 0.8767 mL | 1.7533 mL | 4.3833 mL | |
| 20 mM | 0.1315 mL | 0.6575 mL | 1.3150 mL | 3.2875 mL | |
| 25 mM | 0.1052 mL | 0.5260 mL | 1.0520 mL | 2.6300 mL | |
| 30 mM | 0.0877 mL | 0.4383 mL | 0.8767 mL | 2.1917 mL | |
| 40 mM | 0.0657 mL | 0.3287 mL | 0.6575 mL | 1.6437 mL |
MAPK-IN-2 Related Classifications
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