GDC-0425
Based on 1 Customer Validation
GDC-0425 (RG-7602) is an orally available, highly selective small molecule ChK1 inhibitor. GDC-0425 can be used for the research of various malignancies.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.39%
- No. CAS: 1200129-48-1
- Fòrmula: C18H19N5O
- Peso molecular:321.38
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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Chk1 |
MEK inhibition either by pharmacologic inhibitors or RNAi-mediated gene silencing significantly protected cells from reduced viability upon GDC-0425 treatment[3].
GDC-0425 (3 μM; 24 hours) treatment results the hyperphosphorylation of Chk1[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Chk1-positive breast cancer cell lines
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Concentration:0.001, 0.01, 0.1, 1, 10 mM
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Incubation Time:72 hours
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Result:Reduced cell proliferation.
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Cell Line:U-2 OS cells
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Concentration:3 μM
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Incubation Time:24 hours
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Result:Led to hyperphosphorylation of Chk1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCr nude mice bearing xenografts of both osteosarcoma and triple-negative breast cancer models (143B PML BK TK, HCC1806, and HCC70 cell lines)[3]
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Dosage:For the 4-arm study, mice were treated with vehicle, Gemcitabine 120 mg/kg, GDC-0425 75 mg/kg alone, or Gemcitabine and GDC-0425 combination for 15 days. For 6-arm studies of HCC1806 and HCC70 models, mice were treated with vehicle, Gemcitabine 120 mg/kg, GDC-0425 50 mg/kg, GDC-0425 75 mg/kg alone, or Gemcitabine and GDC-0425 combination.
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Administration:Orally administrated at 24, 48, and 72 hours after gemcitabine administration by intraperitoneal injection.
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Result:Exhibited partial suppression of tumor growth upon treatment with either Gemcitabine or GDC-0425 alone. Notably, the Gemcitabine/GDC-0425 combination resulted in significant tumor regression in all tested models.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1200129-48-1
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Appearance Solid
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Peso molecular 321.38
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Fòrmula C18H19N5O
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Color Off-white to brown
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SMILES
N#CC1=NC=C2C(C3=CC=CN=C3N2)=C1OC4CCN(CC)CC4
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Synonyms
RG-7602
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
H2O : 25 mg/mL (77.79 mM; ultrasonic and adjust pH to 3 with HCl)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Xiao Ding, et al. A supported liquid extraction LC-MS/MS method for determination of concentrations of GDC-0425, a small molecule Checkpoint kinase 1 inhibitor, in human plasma. Biomed Chromatogr. 2016 Dec;30(12):1984-1991. [Content Brief]
[2]. Jeffrey R Infante, et al. Phase I Study of GDC-0425, a Checkpoint Kinase 1 Inhibitor, in Combination with Gemcitabine in Patients with Refractory Solid Tumors. Clin Cancer Res. 2017 May 15;23(10):2423-2432. [Content Brief]
[3]. Ho-June Lee, et al. Ras-MEK Signaling Mediates a Critical Chk1-Dependent DNA Damage Response in Cancer Cells. Mol Cancer Ther. 2017 Apr;16(4):694-704. [Content Brief]
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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 3.1116 mL | 15.5579 mL | 31.1158 mL | 77.7895 mL |
| 5 mM | 0.6223 mL | 3.1116 mL | 6.2232 mL | 15.5579 mL | |
| 10 mM | 0.3112 mL | 1.5558 mL | 3.1116 mL | 7.7790 mL | |
| 15 mM | 0.2074 mL | 1.0372 mL | 2.0744 mL | 5.1860 mL | |
| 20 mM | 0.1556 mL | 0.7779 mL | 1.5558 mL | 3.8895 mL | |
| 25 mM | 0.1245 mL | 0.6223 mL | 1.2446 mL | 3.1116 mL | |
| 30 mM | 0.1037 mL | 0.5186 mL | 1.0372 mL | 2.5930 mL | |
| 40 mM | 0.0778 mL | 0.3889 mL | 0.7779 mL | 1.9447 mL | |
| 50 mM | 0.0622 mL | 0.3112 mL | 0.6223 mL | 1.5558 mL | |
| 60 mM | 0.0519 mL | 0.2593 mL | 0.5186 mL | 1.2965 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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