PROTAC K-Ras Degrader-3
Based on 1 Customer Validation
PROTAC K-Ras Degrader-3 (compound 40) is a PROTAC degrader of K-Ras with a DC50 of ≤ 1 nM against SW620 KRAS G12D, and a GI50 of ≤ 10 nM against SW620 3D cell growth. PROTAC K-Ras Degrader-3 can be utilized in cancer research, such as non-small-cell lung cancer (NSCLC).
(Pink: K-RAS ligand (HY-168056); Blue: Cereblon ligand (HY-168055); Black: linker (HY-168075)).
For research use only. We do not sell to patients.
- Purity: 99.75%
- CAS No.: 3043670-68-1
- Formula: C57H67F2N9O6
- Molecular Weight:1012.20
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Storage:Powder -20°C, 3 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
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Biological Activity
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KRas G12D <1 nM (DC50) |
KRAS G12V/RAF1 <20 nM (IC50) |
| Species | Dose | Route | AUC0-last |
|---|---|---|---|
| Mice | 30 mg/kg | p.o. | 652 ng·h/mL |
Chemical Information
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CAS No. 3043670-68-1
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Appearance Solid
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Molecular Weight 1012.20
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Formula C57H67F2N9O6
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Color White to off-white
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SMILES
FC1=C(CC)C2=C(C3=C(F)C4=NC(OCC5(CC5)CN6CCC(CN7CC8(CCN(C9=CC=C(C(N([C@@H]%10C(NC(CC%10)=O)=O)C%11)=O)C%11=C9)CC8)C7)(C)CC6)=NC(N%12C[C@@](O)(C)CCC%12)=C4C=N3)C=C(O)C=C2C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (98.79 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 (2.47 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 (2.47 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 (269 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 | 0.9879 mL | 4.9397 mL | 9.8795 mL | 24.6987 mL |
| 5 mM | 0.1976 mL | 0.9879 mL | 1.9759 mL | 4.9397 mL | |
| 10 mM | 0.0988 mL | 0.4940 mL | 0.9879 mL | 2.4699 mL | |
| 15 mM | 0.0659 mL | 0.3293 mL | 0.6586 mL | 1.6466 mL | |
| 20 mM | 0.0494 mL | 0.2470 mL | 0.4940 mL | 1.2349 mL | |
| 25 mM | 0.0395 mL | 0.1976 mL | 0.3952 mL | 0.9879 mL | |
| 30 mM | 0.0329 mL | 0.1647 mL | 0.3293 mL | 0.8233 mL | |
| 40 mM | 0.0247 mL | 0.1235 mL | 0.2470 mL | 0.6175 mL | |
| 50 mM | 0.0198 mL | 0.0988 mL | 0.1976 mL | 0.4940 mL | |
| 60 mM | 0.0165 mL | 0.0823 mL | 0.1647 mL | 0.4116 mL | |
| 80 mM | 0.0123 mL | 0.0617 mL | 0.1235 mL | 0.3087 mL |
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