BI-0474
Based on 1 Customer Validation
BI-0474 is a potent KRASG12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models.
For research use only. We do not sell to patients.
The BI-0474 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- Purity: 99.83%
- CAS No.: 2750570-55-7
- Formula: C30H37N9O2S
- Molecular Weight:587.74
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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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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-SOS1 7.0 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LS-513 | EC50 |
>4 μM
Compound: 23; BI-0474
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Antiproliferative activity against human LS-513 cells harboring KRAS G12D mutant incubated for 5 days by celltiter glo luminescent assay
Antiproliferative activity against human LS-513 cells harboring KRAS G12D mutant incubated for 5 days by celltiter glo luminescent assay
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[PMID: 36300829] |
| NCI-H358 | EC50 |
26 nM
Compound: 23; BI-0474
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Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant incubated for 3 days by celltiter glo luminescent assay
Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant incubated for 3 days by celltiter glo luminescent assay
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[PMID: 36300829] |
BI-0474 (1-10,000 nM; 3 days) shows potent antiproliferative activity of 26 nM on NCI-H358 cells carrying a G12C mutation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H358 cells (carrying a G12C mutation)
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Concentration:1-10,000 nM
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Incubation Time:3 days
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Result:Inhibited proliferation of NCI-H358 cells with an EC50 of 26 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NMRI nude mice (NCI-H358 cell line-derived non-small cell lung cancer xenograft model)[1].
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Dosage:40 mg/kg
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Administration:Intraperitoneal administration; single daily for 3 days
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Result:Led to induction of programmed cell death in this xenograft model.
Chemical Information
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CAS No. 2750570-55-7
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Appearance Solid
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Molecular Weight 587.74
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Formula C30H37N9O2S
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Color White to off-white
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SMILES
N#CC1=C(N)SC2=C1[C@@](C)(C3=NC(C4=NC(N5[C@@H](C)CN(C)CC5)=CC(N6CCN(C(C=C)=O)CC6)=C4)=NO3)CCC2
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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 (170.14 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 (4.25 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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 (282 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)
- 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 | 1.7014 mL | 8.5072 mL | 17.0143 mL | 42.5358 mL |
| 5 mM | 0.3403 mL | 1.7014 mL | 3.4029 mL | 8.5072 mL | |
| 10 mM | 0.1701 mL | 0.8507 mL | 1.7014 mL | 4.2536 mL | |
| 15 mM | 0.1134 mL | 0.5671 mL | 1.1343 mL | 2.8357 mL | |
| 20 mM | 0.0851 mL | 0.4254 mL | 0.8507 mL | 2.1268 mL | |
| 25 mM | 0.0681 mL | 0.3403 mL | 0.6806 mL | 1.7014 mL | |
| 30 mM | 0.0567 mL | 0.2836 mL | 0.5671 mL | 1.4179 mL | |
| 40 mM | 0.0425 mL | 0.2127 mL | 0.4254 mL | 1.0634 mL | |
| 50 mM | 0.0340 mL | 0.1701 mL | 0.3403 mL | 0.8507 mL | |
| 60 mM | 0.0284 mL | 0.1418 mL | 0.2836 mL | 0.7089 mL | |
| 80 mM | 0.0213 mL | 0.1063 mL | 0.2127 mL | 0.5317 mL | |
| 100 mM | 0.0170 mL | 0.0851 mL | 0.1701 mL | 0.4254 mL |
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