Kobe2602
Based on 1 publication(s) in Google Scholar
Kobe2602 is a Ras-Raf interaction inhibitor. Kobe2602 inhibits the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki of 149 μM. Kobe2602 has antitumor activity.
For research use only. We do not sell to patients.
- Purity: 98.20%
- CAS No.: 454453-49-7
- Formula: C14H9F4N5O4S
- Molecular Weight:419.31
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Storage:Powder -20°C, 3 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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Kobe2602
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Biological Activity
Ki: 149 μM (Ras-Raf interaction)[1]
Kobe2602 (2-20 μM; 1 hour) exhibits Ras-Raf-binding inhibition in NIH 3T3 cells[1].
Kobe2602 has IC50 value of approximately 10 μM for the cellular Ras-Raf-binding inhibition[1].
Kobe2602 (20 μM) efficiently inhibits the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-RasG12V[1].
Kobe2602 inhibits Ras?GTP but not Ras?GDP[1].
Kobe2602 (20 μM) inhibits the anchorage-dependent proliferation of H-RasG12V-transformed cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H-rasG12V-transformed NIH 3T3 cells
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Concentration:20 μM
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Incubation Time:24 hours , 48 hours, 72 hours
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Result:Efficiently inhibited colony formation in soft agar in a dose-dependent manner.
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Cell Line:NIH 3T3 cells
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Concentration:2 μM, 20 μM
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Incubation Time:1 hour
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Result:Effectively reduced the amount of c-Raf-1 associated with H-RasG12V in NIH 3T3 cells in a dose-dependent manner, indicating the inhibition of the cellular activity of Ras.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic nude mice (6-8 wk old), with SW480 cells xenograft[1]
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Dosage:80 mg/kg
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Administration:Oral administration, five consecutive days per week, for 17 days
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Result:Caused inhibition of the tumor growth.
Chemical Information
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CAS No. 454453-49-7
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Appearance Solid
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Molecular Weight 419.31
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Formula C14H9F4N5O4S
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Color Light yellow to brown
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SMILES
FC(C1=CC([N+]([O-])=O)=C(NNC(NC2=CC=C(F)C=C2)=S)C([N+]([O-])=O)=C1)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : ≥ 250 mg/mL (596.22 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (11.92 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
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 | 2.3849 mL | 11.9244 mL | 23.8487 mL | 59.6218 mL |
| 5 mM | 0.4770 mL | 2.3849 mL | 4.7697 mL | 11.9244 mL | |
| 10 mM | 0.2385 mL | 1.1924 mL | 2.3849 mL | 5.9622 mL | |
| 15 mM | 0.1590 mL | 0.7950 mL | 1.5899 mL | 3.9748 mL | |
| 20 mM | 0.1192 mL | 0.5962 mL | 1.1924 mL | 2.9811 mL | |
| 25 mM | 0.0954 mL | 0.4770 mL | 0.9539 mL | 2.3849 mL | |
| 30 mM | 0.0795 mL | 0.3975 mL | 0.7950 mL | 1.9874 mL | |
| 40 mM | 0.0596 mL | 0.2981 mL | 0.5962 mL | 1.4905 mL | |
| 50 mM | 0.0477 mL | 0.2385 mL | 0.4770 mL | 1.1924 mL | |
| 60 mM | 0.0397 mL | 0.1987 mL | 0.3975 mL | 0.9937 mL | |
| 80 mM | 0.0298 mL | 0.1491 mL | 0.2981 mL | 0.7453 mL | |
| 100 mM | 0.0238 mL | 0.1192 mL | 0.2385 mL | 0.5962 mL |
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