KRAS G12D inhibitor 1
Based on 1 Customer Validation
KRAS G12D inhibitor 1 is a KRASG12D inhibitor with an IC50 value of 0.4 nM. KRAS G12D inhibitor 1 inhibits KRasG12D-mediated ERK phosphorylation. KRAS G12D inhibitor 1 can be used for cancer research.
For research use only. We do not sell to patients.
- CAS No.: 2621928-43-4
- Formula: C33H32F2N6O2
- Molecular Weight:582.64
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
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KRas G12D 0.4 nM (IC50) |
KRASG12D inhibitor 1 (Compound 243) potently inhibits binding to KRASG12D in cell-free biochemical assays, with an IC50 of 0.4 nM[1].
KRASG12D inhibitor 1 potently inhibits KRasG12D-mediated ERK phosphorylation in cell-based assays, with an IC50 of 0.8 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2621928-43-4
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Appearance Solid
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Molecular Weight 582.64
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Formula C33H32F2N6O2
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Color Yellow to brown
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SMILES
OC1=CC(C2=C(F)C3=NC(OC[C@@]45CCCN4C[C@H](F)C5)=NC(N6C[C@H]7N[C@H](CC7)C6)=C3C=N2)=C8C(C#C)=CC=CC8=C1
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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 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (171.63 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)
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 (4.29 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 (4.29 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 (275 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. 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 | 1.7163 mL | 8.5816 mL | 17.1633 mL | 42.9081 mL |
| 5 mM | 0.3433 mL | 1.7163 mL | 3.4327 mL | 8.5816 mL | |
| 10 mM | 0.1716 mL | 0.8582 mL | 1.7163 mL | 4.2908 mL | |
| 15 mM | 0.1144 mL | 0.5721 mL | 1.1442 mL | 2.8605 mL | |
| 20 mM | 0.0858 mL | 0.4291 mL | 0.8582 mL | 2.1454 mL | |
| 25 mM | 0.0687 mL | 0.3433 mL | 0.6865 mL | 1.7163 mL | |
| 30 mM | 0.0572 mL | 0.2861 mL | 0.5721 mL | 1.4303 mL | |
| 40 mM | 0.0429 mL | 0.2145 mL | 0.4291 mL | 1.0727 mL | |
| 50 mM | 0.0343 mL | 0.1716 mL | 0.3433 mL | 0.8582 mL | |
| 60 mM | 0.0286 mL | 0.1430 mL | 0.2861 mL | 0.7151 mL | |
| 80 mM | 0.0215 mL | 0.1073 mL | 0.2145 mL | 0.5364 mL | |
| 100 mM | 0.0172 mL | 0.0858 mL | 0.1716 mL | 0.4291 mL |
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