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.
体外研究
MEK 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.
Cell Viability Assay
Cell 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 Assay
Cell Line:
U-2 OS cells
Concentration:
3 μM
Incubation Time:
24 hours
Result:
Led to hyperphosphorylation of Chk1.
体内研究
GDC-0425 exhibits partial suppression of tumor growth. The Gemcitabine/GDC-0425 combination results in significant tumor regression in all tested models.
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.
分子量
321.38
CAS号
1200129-48-1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
H2O : 25 mg/mL (77.79 mM; ultrasonic and adjust pH to 3 with HCl)