PROTAC K-Ras Degrader-5
Based on 1 Customer Validation
PROTAC K-Ras Degrader-5 is a cereblon-based K-Ras PROTAC degrader with a DC50 of <100 nM for KRASG12D. PROTAC K-Ras Degrader-5 recruits KRASG12D to the cereblon E3 ubiquitin ligase complex for ubiquitination and subsequent proteasomal degradation. PROTAC K-Ras Degrader-5 suppresses pERK levels downstream of KRASG12D degradation in cancer cells. PROTAC K-Ras Degrader-5 reduces proliferation of cancer cells. PROTAC K-Ras Degrader-5 induces caspase 3/7 activity and cPARP, markers of apoptosis, in pancreatic cancer spheroids and tumors. PROTAC K-Ras Degrader-5 can be used for the research of pancreatic cancer and colorectal cancer.
(Pink: K-RAS ligand (HY-168671); Blue: Cereblon E3 ligase ligand; Black: linker).
For research use only. We do not sell to patients.
- Purity: 95.04%
- CAS No.: 3052745-16-8
- Formula: C57H63F3N10O5
- Molecular Weight:1025.17
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Storage:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, 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
Biological Activity
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Cereblon |
KRas G12D <100 nM (DC50) |
Caspase 3 |
Caspase-7 |
PROTAC K-Ras Degrader-5 (compound 69) (0.01-100 nM) inhibits the viability of AsPC-1, Panc04.03, SW1990, Panc08.13, LS180 and A427 cells[1].
PROTAC K-Ras Degrader-5 (0.01-1000 nM; 24-96 h) suppresses the level of pERK in AsPC-1 spheroids[1].
PROTAC K-Ras Degrader-5 (0.5-4 nM; 16 h) induces caspase 3/7 activity in pancreatic cancer spheroids[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PROTAC K-Ras Degrader-5 AsPC-1 (0.3-3 mg/kg; i.v.; twice weekly; once weekly; once every two weeks) effectively inhibits tumor growth in AsPC-1, SW1990, HPAC and Panc04.03 pancreatic cancer xenograft mouse models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB17 SCID female mice (6-8 weeks old) were subcutaneously injected with GP2d colorectal cancer cells[1]
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Dosage:1 mg/kg, 3 mg/kg
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Administration:i.v.; twice weekly; once weekly; once every two weeks
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Result:Led to 93-102% tumor growth inhibition (TGI).
Chemical Information
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CAS No. 3052745-16-8
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Appearance Solid
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Molecular Weight 1025.17
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Formula C57H63F3N10O5
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Color Off-white to light yellow
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SMILES
C#CC1=C(C=CC2=CC(O)=CC(C3=C(C4=NC(OCCN5CCC(CC5)CC6CCN(CC6)CC7CCN(CC7)C8=CC=C9C(N(CC9=C8F)C%10CCC(NC%10=O)=O)=O)=NC(N%11C[C@H]%12N[C@H](CC%12)C%11)=C4C=N3)F)=C21)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (97.54 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 (protect from light, 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 (protect from light, 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)
Purity & Documentation
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Data Sheet (270 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 (protect from light, 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 |
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| DMSO | 1 mM | 0.9754 mL | 4.8772 mL | 9.7545 mL | 24.3862 mL |
| 5 mM | 0.1951 mL | 0.9754 mL | 1.9509 mL | 4.8772 mL | |
| 10 mM | 0.0975 mL | 0.4877 mL | 0.9754 mL | 2.4386 mL | |
| 15 mM | 0.0650 mL | 0.3251 mL | 0.6503 mL | 1.6257 mL | |
| 20 mM | 0.0488 mL | 0.2439 mL | 0.4877 mL | 1.2193 mL | |
| 25 mM | 0.0390 mL | 0.1951 mL | 0.3902 mL | 0.9754 mL | |
| 30 mM | 0.0325 mL | 0.1626 mL | 0.3251 mL | 0.8129 mL | |
| 40 mM | 0.0244 mL | 0.1219 mL | 0.2439 mL | 0.6097 mL | |
| 50 mM | 0.0195 mL | 0.0975 mL | 0.1951 mL | 0.4877 mL | |
| 60 mM | 0.0163 mL | 0.0813 mL | 0.1626 mL | 0.4064 mL | |
| 80 mM | 0.0122 mL | 0.0610 mL | 0.1219 mL | 0.3048 mL |
PROTAC K-Ras Degrader-5 Related Classifications
HY-168669 Related Classifications
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