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: ligand (HY-168671); Blue: Cereblon E3 ligase ligand; Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 95.04%
- CAS 番号: 3052745-16-8
- 分子式: C57H63F3N10O5
- 分子量:1025.17
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保管条件:
-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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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
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Cereblon |
KRas G12D <100 nM (DC50) |
Caspase 3 |
Caspase-7 |
体外実験
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.
体内実験
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).
化学情報
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CAS 番号 3052745-16-8
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性状 Solid
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分子量 1025.17
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Working solution concentration: 0.22 mg/mL
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
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 関連分類
HY-168669 関連分類
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