(R)-G12Di-7
Based on 1 Customer Validation
(R)-G12Di-7 is a covalent ligand for KRAS-G12D, which selectively labels K-Ras-G12D·GDP and K-Ras-G12D·GppNHp. (R)-G12Di-7 exhibits inhibitory activity against G12D mutated cancer cells.
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- Pureté: 98.42%
- CAS No.: 2946593-60-6
- Formule: C39H37F3N6O5
- Masse moléculaire:726.74
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
(R)-G12Di-7 (1-100 nM) inhibits cell viability in KRAS-G12D mutated cells Ba/F3, SW1990, AsPC-1 and AGS with GI50s of 73 nM, 409 nM, 467 nM and 109 nM, respectively[1].
(R)-G12Di-7 (10 μM) labels KRAS-G12D in G12D mutated cells Ba/F3, SW1990, AsPC-1 and AGS, and thus suppresses the downstream signaling with stability over 12 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3, SW1990, AsPC-1, AGS
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Concentration:1-1000 nM
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Incubation Time:72 h
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Result:Inhibited cell growth of Ba/F3, SW1990, AsPC-1 and AGS.
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Cell Line:Ba/F3, SW1990, AsPC-1, AGS
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Concentration:10 μM
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Incubation Time:4 h
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Result:Suppressed expression K-RAS-G12D and phosphorylation of ERK and Akt in cells G12D mutated cells Ba/F3, SW1990, AsPC-1 and AGS.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SW1900 xenograft NOD/SCID mice[1]
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Dosage:10-50 mg/kg
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Administration:i.p., twice a day for 28 days
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Result:Inhibited tumor growth and weight loss.
Chemical Information
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CAS No. 2946593-60-6
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Appearance Solid
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Masse moléculaire 726.74
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Formule C39H37F3N6O5
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Color White to light yellow
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SMILES
C#CC1=C(C=CC2=CC(O)=CC(C3=C(C4=C(C(N5CC6CCC(N6C([C@@H]7OC(C7(C)C)=O)=O)C5)=NC(OC[C@@]89CCCN8C[C@@H](C9)F)=N4)C=N3)F)=C21)F
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 50 mg/mL (68.80 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)
Pureté et documentation
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Fiche technique (281 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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Instruction de manipulation (2659 KB)
Références
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 | 1.3760 mL | 6.8800 mL | 13.7601 mL | 34.4002 mL |
| 5 mM | 0.2752 mL | 1.3760 mL | 2.7520 mL | 6.8800 mL | |
| 10 mM | 0.1376 mL | 0.6880 mL | 1.3760 mL | 3.4400 mL | |
| 15 mM | 0.0917 mL | 0.4587 mL | 0.9173 mL | 2.2933 mL | |
| 20 mM | 0.0688 mL | 0.3440 mL | 0.6880 mL | 1.7200 mL | |
| 25 mM | 0.0550 mL | 0.2752 mL | 0.5504 mL | 1.3760 mL | |
| 30 mM | 0.0459 mL | 0.2293 mL | 0.4587 mL | 1.1467 mL | |
| 40 mM | 0.0344 mL | 0.1720 mL | 0.3440 mL | 0.8600 mL | |
| 50 mM | 0.0275 mL | 0.1376 mL | 0.2752 mL | 0.6880 mL | |
| 60 mM | 0.0229 mL | 0.1147 mL | 0.2293 mL | 0.5733 mL |