KRas G12R inhibitor 1
Based on 1 Customer Validation
KRas G12R inhibitor 1 is a covalent inhibitor targeting the common oncogenic mutant KRas G12R with selectivity for the mutant arginine. KRas G12R inhibitor 1 possesses an α,β-diketoamide and exploits strong nucleophilicity of the mutant cysteine and irreversibly binds in the Switch II region of KRas. KRas G12R inhibitor 1 can be researched for K-Ras (G12R)-driven cancer such as pancreatic ductal adenocarcinoma (PDAC).
For research use only. We do not sell to patients.
- Purity: 98.40%
- Formula: C39H38ClF7N6O9
- Molecular Weight:903.20
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
Biological Activity
KRas G12R inhibitor 1 (Compound 3) (50 μM, 72 h) results in time-dependent covalent modification of wildtype KRas and KRas G12R[1].
KRas G12R inhibitor 1 (50 μM, 16 h) does not modify hotspot mutants including G12D, G12V, Q61R, Q61K, and Q61L upon extended incubation at pH 7.5[1].
KRas G12R inhibitor 1 (50 μM, 50 h) leads to a pH-dependent reaction with a maximum rate at pH 8 and greatly reduced rate at pH 6[1].
KRas G12R inhibitor 1 (1 h) inhibits Sos-mediated exchange and significantly reduces the rate of EDTA-mediated exchange[1].
KRas G12R inhibitor 1 (100 μM, 16 h) results in complete modification of this exogenous protein after 16 h incubation with recombinant K-Ras G12R in lysates of BaF3/KRas[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Molecular Weight 903.20
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Formula C39H38ClF7N6O9
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Color White to off-white
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SMILES
CC(C(O)(O)C(N1[C@@H]2CC[C@H]1CN(C3=NC(OCC45CCCN4CCC5)=NC6=C3C=NC(C7=C8C(Cl)=CC=CC8=CC=C7)=C6F)C2)=O)=O.FC(F)(F)C(O)=O.FC(F)(F)C(O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (110.72 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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: ≥ 2.5 mg/mL (2.77 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 (2.77 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (279 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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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 (sealed storage, away from moisture). 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 | 1.1072 mL | 5.5359 mL | 11.0717 mL | 27.6794 mL |
| 5 mM | 0.2214 mL | 1.1072 mL | 2.2143 mL | 5.5359 mL | |
| 10 mM | 0.1107 mL | 0.5536 mL | 1.1072 mL | 2.7679 mL | |
| 15 mM | 0.0738 mL | 0.3691 mL | 0.7381 mL | 1.8453 mL | |
| 20 mM | 0.0554 mL | 0.2768 mL | 0.5536 mL | 1.3840 mL | |
| 25 mM | 0.0443 mL | 0.2214 mL | 0.4429 mL | 1.1072 mL | |
| 30 mM | 0.0369 mL | 0.1845 mL | 0.3691 mL | 0.9226 mL | |
| 40 mM | 0.0277 mL | 0.1384 mL | 0.2768 mL | 0.6920 mL | |
| 50 mM | 0.0221 mL | 0.1107 mL | 0.2214 mL | 0.5536 mL | |
| 60 mM | 0.0185 mL | 0.0923 mL | 0.1845 mL | 0.4613 mL | |
| 80 mM | 0.0138 mL | 0.0692 mL | 0.1384 mL | 0.3460 mL | |
| 100 mM | 0.0111 mL | 0.0554 mL | 0.1107 mL | 0.2768 mL |
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