GDC-0994 Chemical Properties

Boiling point:

734.6±70.0 °C(Predicted)

Density 

1.45±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

≥44.1 mg/mL in DMSO; insoluble in H2O; ≥19.2 mg/mL in EtOH

form 

solid

pka

14.03±0.10(Predicted)

color 

White to yellow

Safety Information

HS Code 

2933998090

GDC-0994 Usage And Synthesis

Description

GDC-0994 is a potent and selective ERK1 and ERK2 inhibitor with IC₅₀ values of 6.1 and 4.1 nM, respectively. It inhibits ERK-dependent p90RSK serine 380 phosphorylation in PMA-stimulated HepG2 cells with an IC₅₀ value of 12 nM. GDC-0994 inhibited growth of HCT116 human colorectal cancer xenograft tumors by 49%, 57%, and 80% at 30, 60, and 100 mg/kg, respectively, when administered orally once daily for 21 days.

Uses

GDC-0994 is a potent and orally available ERK12 inhibitor shown to prevent ERK-dependant tumor cell proliferation and survival.

References

[1]. robarge k, schwarz j, blake j, et al. abstract ddt02-03: discovery of gdc-0994, a potent and selective erk1/2 inhibitor in early clinical development. aacr annual meeting, 2014, san diego, ca.