PROTAC K-Ras Degrader-1
Based on 2 publication(s) in Google Scholar
PROTAC K-Ras Degrader-1 is a K-Ras PROTAC degrader. It binds to both K-Ras and the Cereblon E3 ubiquitin ligase, bringing K-Ras into proximity with the ligase, thereby achieving its degradation and inhibition. PROTAC K-Ras Degrader-1 can be used for research in various cancers.
(Pink: Target protein ligand; Blue: Cereblon ligand (HY-14658); Black: linker (HY-187068)).
For research use only. We do not sell to patients.
- Purity : 99.90%
- CAS No.: 2378258-52-5
- Formula: C53H62N10O10
- Molecular Weight:999.12
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Storage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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
Publications Citing Use of MedChemExpress (MCE) PROTAC K-Ras Degrader-1
MoreAll PROTACs Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
KRAS(G12C) |
Cereblon |
MCE Validation Data
In Vitro
PROTAC K-Ras Degrader-1 (compound 518) induces K-Ras ubiquitination and proteasomal degradation in cancer cells by recruiting ubiquitin ligases, accompanied by an electrophoretic mobility shift resulting from covalent modification[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. 2378258-52-5
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Appearance Solid
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Molecular Weight 999.12
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Formula C53H62N10O10
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Color Light yellow to yellow
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SMILES
CN1[C@@H](C[C@@H](OCCOCCOCCOCCNC2=C3C(C(N(C4C(NC(CC4)=O)=O)C3=O)=O)=CC=C2)C1)COC5=NC(N6C[C@@H](N(C(C=C)=O)CC6)CC#N)=C7C(CN(C8=CC=CC9=C8C=CC=C9)CC7)=N5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (2)
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Journal Impact Factor
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Most Recent
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Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062 -
Solvent & Solubility
In Vitro:
DMSO : 33.33 mg/mL (33.36 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 (stored under nitrogen). 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 (stored under nitrogen). 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)
In Vivo:
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 (2.50 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 (2.50 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.
In Vivo Dissolution Calculator
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 (stored under nitrogen)
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 (288 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)
- Korean - KR (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 (stored under nitrogen). 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 | 1.0009 mL | 5.0044 mL | 10.0088 mL | 25.0220 mL |
| 5 mM | 0.2002 mL | 1.0009 mL | 2.0018 mL | 5.0044 mL | |
| 10 mM | 0.1001 mL | 0.5004 mL | 1.0009 mL | 2.5022 mL | |
| 15 mM | 0.0667 mL | 0.3336 mL | 0.6673 mL | 1.6681 mL | |
| 20 mM | 0.0500 mL | 0.2502 mL | 0.5004 mL | 1.2511 mL | |
| 25 mM | 0.0400 mL | 0.2002 mL | 0.4004 mL | 1.0009 mL | |
| 30 mM | 0.0334 mL | 0.1668 mL | 0.3336 mL | 0.8341 mL |
PROTAC K-Ras Degrader-1 Related Classifications
HY-129523 Related Classifications
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