GDC-0425 (C09-1135-810)

GDC-0425 (RG-7602) is an orally available, highly selective small molecule ChK1 inhibitor. GDC-0425 can be used for the research of various malignanciesIn VitroMEK inhibition either by pharmacologic inhibitors or RNAi-mediated gene silencing significantly protected cells from reduced viability upon GDC-0425 treatment. GDC-0425 (3 μM; 24 hours) treatment results the hyperphosphorylation of Chk1. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Chk1-positive breast cancer cell lines Concentration: 0.001, 0.01, 0.1, 1, 10 mM Incubation Time: 72 hours Result: Reduced cell proliferation. Cell Viability AssayCell Line: U-2 OS cells Concentration: 3 μM Incubation Time: 24 hours Result: Led to hyperphosphorylation of Chk1.In VivoGDC-0425 exhibits partial suppression of tumor growth. The Gemcitabine/GDC-0425 combination results in significant tumor regression in all tested models. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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)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.Form:SolidIC50& Target:Chk1. Specification: 0.99 Molecular Formula: C18H19N5O Molecular Weight: 321.38