K-Ras G12C-IN-4
Based on 1 Customer Validation
K-Ras G12C-IN-4, compound 1, is a potent Covalent Inhibitor of KRASG12C.
For research use only. We do not sell to patients.
- Purity: 99.19%
- CAS No.: 2376328-55-9
- Formula: C31H33ClN4O4
- Molecular Weight:561.07
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Storage: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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
>10 μM
Compound: 1
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Inhibition of KRAS G12C mutant in human A549 cells assessed as reduction in EGF-induced ERK1/2 phosphorylation incubated for 4 hrs followed by EGF addition by luminescence based assay
Inhibition of KRAS G12C mutant in human A549 cells assessed as reduction in EGF-induced ERK1/2 phosphorylation incubated for 4 hrs followed by EGF addition by luminescence based assay
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[PMID: 31531201] |
| A549 | IC50 |
9.33 μM
Compound: 1
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Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay
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[PMID: 31531201] |
| MIA PaCa-2 | IC50 |
0.067 μM
Compound: 1
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Cytotoxicity against human MIAPaCa2 cells assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay
Cytotoxicity against human MIAPaCa2 cells assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay
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[PMID: 31531201] |
K-Ras G12C-IN-4 (4 hours) exhibits IC50=0.219 μM for inhibition of MAPK signaling (p-ERK) in MIA PaCa-2 cells[1]. K-Ras G12C-IN-4 (72 hours) translates to a 0.067 μM IC50 for inhibition of cellular viability in a CellTiter-Glo experiment in MIA PaCa-2 cells[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. 2376328-55-9
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Appearance Solid
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Molecular Weight 561.07
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Formula C31H33ClN4O4
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Color White to off-white
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SMILES
O=C(NC1CN(C(C=C)=O)C1)CN2C(C3CC3)=C(C(N4CC5=C(C(OC)=CC=C5)CC4)=O)C6=C2C(C)=CC(Cl)=C6
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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 : 62.5 mg/mL (111.39 mM; ultrasonic and warming and heat to 60°C; 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 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.71 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (274 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7823 mL | 8.9115 mL | 17.8231 mL | 44.5577 mL |
| 5 mM | 0.3565 mL | 1.7823 mL | 3.5646 mL | 8.9115 mL | |
| 10 mM | 0.1782 mL | 0.8912 mL | 1.7823 mL | 4.4558 mL | |
| 15 mM | 0.1188 mL | 0.5941 mL | 1.1882 mL | 2.9705 mL | |
| 20 mM | 0.0891 mL | 0.4456 mL | 0.8912 mL | 2.2279 mL | |
| 25 mM | 0.0713 mL | 0.3565 mL | 0.7129 mL | 1.7823 mL | |
| 30 mM | 0.0594 mL | 0.2971 mL | 0.5941 mL | 1.4853 mL | |
| 40 mM | 0.0446 mL | 0.2228 mL | 0.4456 mL | 1.1139 mL | |
| 50 mM | 0.0356 mL | 0.1782 mL | 0.3565 mL | 0.8912 mL | |
| 60 mM | 0.0297 mL | 0.1485 mL | 0.2971 mL | 0.7426 mL | |
| 80 mM | 0.0223 mL | 0.1114 mL | 0.2228 mL | 0.5570 mL | |
| 100 mM | 0.0178 mL | 0.0891 mL | 0.1782 mL | 0.4456 mL |
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