GDC-0425

Research use only, not for human use.

A potent, selective and orally active Chk1 inhibitor; enhances gemcitabine efficacy in tumor xenograft models.

A potent, selective and orally active Chk1 inhibitor; enhances gemcitabine efficacy in tumor xenograft models; shows greater chemopotentiation in cancer cell lines lacking p53 activity.Solid Tumors Phase 1 Discontinued.

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.

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.

RG-7602 | RG7602 | GDC0425

Angiogenesis

Chk

Chk

Cancer

Solid Tumors

1200129-48-1

321.384

C18H19N5O

>98% (HPLC)

In Vitro:?H2O : 25 mg/mL (77.79 mM助)

N#CC1=NC=C2C(C3=CC=CN=C3N2)=C1OC4CCN(CC)CC4

5-((1-ethylpiperidin-4-yl)oxy)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years