| Identification | Back Directory | [Name]
GDC-0425 | [CAS]
1200129-48-1 | [Synonyms]
RG7602
RG-7602
GDC-0425
5-(1-ethylpiperidin-4-yloxy)-9H-dipyrido[2,3-b-4',3'-d]pyrrole-6-carbonitrile
5-((1-ethylpiperidin-4-yl)oxy)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile | [Molecular Formula]
C18H19N5O | [MDL Number]
MFCD31536987 | [MOL File]
1200129-48-1.mol | [Molecular Weight]
321.38 |
| Chemical Properties | Back Directory | [Boiling point ]
589.2±50.0 °C(Predicted) | [density ]
1.33±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
10.73±0.50(Predicted) | [color ]
Off-white to brown | [Water Solubility ]
Water : 25 mg/mL (77.79 mM; ultrasonic and adjust pH to 3 with HCl) |
| Hazard Information | Back Directory | [Uses]
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[1][2]. | [in vivo]
GDC-0425 exhibits partial suppression of tumor growth. The Gemcitabine/GDC-0425 combination results in significant tumor regression in all tested models[3]. | 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] | | 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. | | Administration: | Orally administrated at 24, 48, and 72 hours after gemcitabine administration by intraperitoneal injection. | | 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.
|
| [IC 50]
Chk1 | [storage]
Store at -20°C | [References]
[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. DOI:10.1002/bmc.3775
[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. DOI:10.1158/1078-0432.CCR-16-1782
[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. DOI:10.1158/1535-7163.MCT-16-0504 |
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| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
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