Pan KRas-IN-1
Based on 1 publication(s) in Google Scholar
Pan KRas-IN-1 is a pan KRas inhibitor, can be used for agent resistance in cancer developed with KRas G12C inhibitors.
For research use only. We do not sell to patients.
- Purity: 99.31%
- CAS No.: 2791263-84-6
- Formula: C33H36F3N5O3
- Molecular Weight:607.67
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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
Publications Citing Use of MedChemExpress (MCE) Pan KRas-IN-1
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Biological Activity
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KRas G12D ≤2 nM (IC50) |
KRas G12S ≤2 nM (IC50) |
KRas G12C ≤2 nM (IC50) |
KRas Q61H ≤2 nM (IC50) |
KRas G12V ≤2 nM (IC50) |
K-Ras WT ≤2 nM (IC50) |
K-Ras G12R ≤2 nM (IC50) |
K-Ras G13D ≤2 nM (IC50) |
K-Ras G12A ≤2 nM (IC50) |
Pan KRas-IN-1 (example 5) shows high binding capacity to KRas, with IC50s of <2 nM among different KRas isform, including G12D, G12V, G12R, G12A, G12S, G13D, Q61H, and WT[1].
Pan KRas-IN-1 inhibits the phosphorylation of ERK downstream of KRas in different cells; AsPC-1 (G12D, IC50=9 nM), A549 (G12S, IC50=11 nM), HCT116 (G13D, IC50=23 nM), NCI-H358 (G12C, IC50=6 nM), NCI-H460 (Q61H, IC50=12 nM), NCI-H727 (G12V, IC50=29 nM), MKN1 (WT, IC50=32 nM), PSN-1 (G12R, IC50=681 nM)[1].
Pan KRas-IN-1 (0-3000 nM; 5 d) exhibits anti-proliferative activity against mutation of reststance to Adagrasib (HY-130149, MRTX849) in mouse 3T3 fibroblasts, with IC50s of 32 nM (G12A), 28.1 nM (G12C), 20.25 nM (G12D), 1742 nM (G12R), 94 nM (G12V), 50 nM (G12W), 610 nM (G13D), 58 nM (Q61H)[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. 2791263-84-6
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Appearance Solid
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Molecular Weight 607.67
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Formula C33H36F3N5O3
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Color Off-white to light yellow
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SMILES
FC1=C(C2=CC(O)=CC3=C2C(CC)=C(F)C=C3)N=CC4=C1N=C(N=C4N5C[C@](O)(CCC5)C)OC[C@@]67N(CCC7)C[C@@H](C6)F
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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 and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Ann Oncol
Genomic landscape of clinically acquired resistance alterations in patients treated with KRASG12C inhibitors. [Abstract]2025 Jun;36(6):682-692. PMID: 39914665
Solvent & Solubility
DMSO : 100 mg/mL (164.56 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 and light). 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 and light). 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 (4.11 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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 (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 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 and light). 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 | 1.6456 mL | 8.2282 mL | 16.4563 mL | 41.1408 mL |
| 5 mM | 0.3291 mL | 1.6456 mL | 3.2913 mL | 8.2282 mL | |
| 10 mM | 0.1646 mL | 0.8228 mL | 1.6456 mL | 4.1141 mL | |
| 15 mM | 0.1097 mL | 0.5485 mL | 1.0971 mL | 2.7427 mL | |
| 20 mM | 0.0823 mL | 0.4114 mL | 0.8228 mL | 2.0570 mL | |
| 25 mM | 0.0658 mL | 0.3291 mL | 0.6583 mL | 1.6456 mL | |
| 30 mM | 0.0549 mL | 0.2743 mL | 0.5485 mL | 1.3714 mL | |
| 40 mM | 0.0411 mL | 0.2057 mL | 0.4114 mL | 1.0285 mL | |
| 50 mM | 0.0329 mL | 0.1646 mL | 0.3291 mL | 0.8228 mL | |
| 60 mM | 0.0274 mL | 0.1371 mL | 0.2743 mL | 0.6857 mL | |
| 80 mM | 0.0206 mL | 0.1029 mL | 0.2057 mL | 0.5143 mL | |
| 100 mM | 0.0165 mL | 0.0823 mL | 0.1646 mL | 0.4114 mL |
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