K-Ras-IN-1
Based on 1 Customer Validation
K-Ras-IN-1 is the inhibitor for K-Ras by occupying the binding site of son of sevenless (Sos), preventing the interaction between Sos and K-Ras, inhibiting the Sos-catalyzed GDP to GTP exchange process. K-Ras-IN-1 is promising for research of pancreatic, colon and lung cancer.
For research use only. We do not sell to patients.
- Purity: 98.00%
- CAS No.: 84783-01-7
- Formula: C11H13NOS
- Molecular Weight:207.29
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Storage: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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
K-Ras[1]
K-Ras-IN-1 binds to K-Ras (WT), K-Ras (G12D), K-Ras (G12V), and H-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure[2].
K-Ras-IN-1 binds to GDP-bound K-Ras (G12D) with an affinity of 1.3-2 mM[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. 84783-01-7
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Appearance Solid
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Molecular Weight 207.29
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Formula C11H13NOS
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Color White to off-white
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SMILES
S=C(C1=CC=CC=C1O)N2CCCC2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 100 mg/mL (482.42 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 (12.06 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 (12.06 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.
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 (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)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Hocker HJ, et al. LIBSA--a method for the determination of ligand-binding preference to allosteric sites on receptor ensembles. J Chem Inf Model. 2014 Feb 24;54(2):530-538. [Content Brief]
[2]. Sun Q, et al. Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation. Angew Chem Int Ed Engl. 2012 Jun 18;51(25):6140-3. [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 | 4.8242 mL | 24.1208 mL | 48.2416 mL | 120.6040 mL |
| 5 mM | 0.9648 mL | 4.8242 mL | 9.6483 mL | 24.1208 mL | |
| 10 mM | 0.4824 mL | 2.4121 mL | 4.8242 mL | 12.0604 mL | |
| 15 mM | 0.3216 mL | 1.6081 mL | 3.2161 mL | 8.0403 mL | |
| 20 mM | 0.2412 mL | 1.2060 mL | 2.4121 mL | 6.0302 mL | |
| 25 mM | 0.1930 mL | 0.9648 mL | 1.9297 mL | 4.8242 mL | |
| 30 mM | 0.1608 mL | 0.8040 mL | 1.6081 mL | 4.0201 mL | |
| 40 mM | 0.1206 mL | 0.6030 mL | 1.2060 mL | 3.0151 mL | |
| 50 mM | 0.0965 mL | 0.4824 mL | 0.9648 mL | 2.4121 mL | |
| 60 mM | 0.0804 mL | 0.4020 mL | 0.8040 mL | 2.0101 mL | |
| 80 mM | 0.0603 mL | 0.3015 mL | 0.6030 mL | 1.5075 mL | |
| 100 mM | 0.0482 mL | 0.2412 mL | 0.4824 mL | 1.2060 mL |
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