SHOC2-RAS PPI-IN-1
Based on 1 Customer Validation
SHOC2-RAS PPI-IN-1 is a SHOC2-NRAS interaction inhibitor with IC50 of 0.048 μM and a Kd of 0.065 μM for SHOC2. SHOC2-RAS PPI-IN-1 inhibits RAS/MAPK signalling and downregulates MEK and ERK phosphorylation. SHOC2-RAS PPI-IN-1 can inhibit cells proliferation in RAS-mutant cancer models. SHOC2-RAS PPI-IN-1 can be used for the research of RAS-mutant cancers.
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- Purity: 99.50%
- 화학식: C20H19IN2O5
- 분자량:494.28
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
All MEK Isoforms
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Biological Activity
제품 설명
IC50 & Target
[1]|
N-Ras (Q61L) |
In Vitro
SHOC2-RAS PPI-IN-1 (Compound 6) (0.01-100 μM) selectively disrupts SHOC2–NRASQ61mut interactions[1].
SHOC2-RAS PPI-IN-1 (1-100 μM, 2-48 h) inhibits oncogenic signalling by decreasing MEK and ERK phosphorylation in MELJUSO cells[1].
SHOC2-RAS PPI-IN-1 (30 μM; 3 weeks) suppresses spheroid growth in MELJUSO cells (NRASQ61L)[1].
SHOC2-RAS PPI-IN-1 (30 μM; 3 weeks) does not suppress spheroid growth in A375 cells (BRAFV600E)[1].
SHOC2-RAS PPI-IN-1 (30-100 μM; 4-24 h) inhibits RAS/MAPK-associated gene (DUSP4, DUSP5, EGR1, SPRY4 and FOSL1) expression in MELJUSO cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MELJUSO cells
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Concentration:1, 10, 30 and 100 μM
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Incubation Time:2, 4, 8, 24 and 48 h
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Result:Reduced MEK and ERK phosphorylation.
Increased RAF(phospho-S259) levles.
Chemical Information
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Appearance Solid
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분자량 494.28
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화학식 C20H19IN2O5
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Color White to off-white
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SMILES
O=C(O)C(C)(C)[C@H](NC(CC1=CC=CC(I)=C1)=O)C2=CC=C(OC(N3)=O)C3=C2
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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 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (202.31 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, 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)
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 (5.06 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 (5.06 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.
순도&문서
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Data Sheet (276 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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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, 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 |
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| DMSO | 1 mM | 2.0231 mL | 10.1157 mL | 20.2314 mL | 50.5786 mL |
| 5 mM | 0.4046 mL | 2.0231 mL | 4.0463 mL | 10.1157 mL | |
| 10 mM | 0.2023 mL | 1.0116 mL | 2.0231 mL | 5.0579 mL | |
| 15 mM | 0.1349 mL | 0.6744 mL | 1.3488 mL | 3.3719 mL | |
| 20 mM | 0.1012 mL | 0.5058 mL | 1.0116 mL | 2.5289 mL | |
| 25 mM | 0.0809 mL | 0.4046 mL | 0.8093 mL | 2.0231 mL | |
| 30 mM | 0.0674 mL | 0.3372 mL | 0.6744 mL | 1.6860 mL | |
| 40 mM | 0.0506 mL | 0.2529 mL | 0.5058 mL | 1.2645 mL | |
| 50 mM | 0.0405 mL | 0.2023 mL | 0.4046 mL | 1.0116 mL | |
| 60 mM | 0.0337 mL | 0.1686 mL | 0.3372 mL | 0.8430 mL | |
| 80 mM | 0.0253 mL | 0.1264 mL | 0.2529 mL | 0.6322 mL | |
| 100 mM | 0.0202 mL | 0.1012 mL | 0.2023 mL | 0.5058 mL |
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