Kobe0065
Based on 4 publication(s) in Google Scholar
Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.
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- Purity: 99.93%
- CAS No.: 436133-68-5
- 화학식: C15H11ClF3N5O4S
- 분자량:449.79
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Kobe0065
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Customer Validation & Images
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Biological Activity
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H-Ras |
Kobe0065-family compounds bind to Ras•GTP and exhibit antiproliferative activity toward cancer cells carrying the activated ras oncogenes. The compounds efficiently inhibit the interaction of Ras•GTP with their multiple effectors including Raf, PI3K, and RalGDS and a regulator/effector Sos and show rather broad binding specificity toward various Ras family small GTPases, which may account for their higher potency at the cellular level compared with that of the in vitro binding inhibition[1]. The phosphorylation of downstream kinases MEK and ERK is effectively attenuated by 20 μM Kobe0065 and Kobe2602 in NIH3T3 cells transiently expressing H-RasG12V[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 436133-68-5
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Appearance Solid
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분자량 449.79
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화학식 C15H11ClF3N5O4S
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Color Light yellow to yellow
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SMILES
FC(C1=CC([N+]([O-])=O)=C(NNC(NC2=CC=C(C)C(Cl)=C2)=S)C([N+]([O-])=O)=C1)(F)F
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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BMC Biol
2022 Dec 13;20(1):278. PMID: 36514097
Kobe0065 purchased from MedChemExpress. Usage Cited in: BMC Biol. 2022 Dec 13;20(1):278. [Abstract]
Kobe0065 (4 μg/each; single) reduces p-ERK levels in the corpora allata (CA), showing the blockage of Ras-Raf interaction, and also results in a significant reduction in JHAMT protein levels, in German cockroach.
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Cell Signal
Cell confluence induces switching from proliferation to migratory signaling by site-selective phosphorylation of PDGF receptors on lipid raft platforms. [Abstract]2016 Feb;28(2):81-93. PMID: 26631574 -
Respir Physiol Neurobiol
The Cosmc-mediated effects of neutrophil elastase on T antigen expression in BEAS-2B cells. [Abstract]2020 Oct;281:103496. PMID: 32683071 -
용액&용해도
DMSO : ≥ 42.5 mg/mL (94.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.56 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.
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.
Protocol
Cells (2×103) are seeded in a 96-well plate and cultured in DMEM containing 2% (vol/vol) FBS in the presence of one of the compounds. Viable cell numbers are measured by formazan formation using a Cell Counting Kit 8. Apoptotic cells are detected by a standard TUNEL assay using an In Situ Cell Detection kit.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cells (5×106) are implanted into the right flanks of female athymic nude mice (6-8 wk old). After tumor sizes reached appr 50 mm3 on average, compounds suspended in Cremophor:ethanol:water (1:1:6) are administered orally for five consecutive days per week for 17 d. Tumor volumes (V) are calculated. Dissected tumors after 17-d administration of the 80 mg/kg compounds are fixed in 4% (wt/vol) paraformaldehyde and embedded in paraffin. Their sections are subjected to immunohistochemistry with an anti-ERK1/2 antibody or an anti-CD31 antibody using a HISTMOUSE-PLUS kit. Apoptotic cells are detected by a TUNEL assay. Statistical significance for groups of three or more is determined by one-way ANOVA with Tukey’s test for post hoc analysis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (277 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)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Shima, Fumi, et al. In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction. Proceedings of the National Academy of Sciences of the United States of America (2013), 110(20), 8182-8187, [Content Brief]
[2]. Shima F, et al. Discovery of small-molecule Ras inhibitors that display antitumor activity by interfering with Ras·GTP-effector interaction. Enzymes. 2013;34 Pt. B:1-23 [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 | 2.2233 mL | 11.1163 mL | 22.2326 mL | 55.5815 mL |
| 5 mM | 0.4447 mL | 2.2233 mL | 4.4465 mL | 11.1163 mL | |
| 10 mM | 0.2223 mL | 1.1116 mL | 2.2233 mL | 5.5581 mL | |
| 15 mM | 0.1482 mL | 0.7411 mL | 1.4822 mL | 3.7054 mL | |
| 20 mM | 0.1112 mL | 0.5558 mL | 1.1116 mL | 2.7791 mL | |
| 25 mM | 0.0889 mL | 0.4447 mL | 0.8893 mL | 2.2233 mL | |
| 30 mM | 0.0741 mL | 0.3705 mL | 0.7411 mL | 1.8527 mL | |
| 40 mM | 0.0556 mL | 0.2779 mL | 0.5558 mL | 1.3895 mL | |
| 50 mM | 0.0445 mL | 0.2223 mL | 0.4447 mL | 1.1116 mL | |
| 60 mM | 0.0371 mL | 0.1853 mL | 0.3705 mL | 0.9264 mL | |
| 80 mM | 0.0278 mL | 0.1390 mL | 0.2779 mL | 0.6948 mL |
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