| Identification | Back Directory | [Name]
GDC-0994 | [CAS]
1453848-26-4 | [Synonyms]
CS-1841
GDC-0994
EOS-60648
Ravoxertinib
GDC-0994;RAVOXERTINIB
RAVOXERTINIB (GDC-0994)
GDC 0994;GDC-0994;GDC0994
(S)-1-(1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one
1-[(1S)-1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl]-2(1H)-pyridinone
2(1H)-Pyridinone, 1-[(1S)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl]-
(S)-1-(1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one GDC-0994 | [Molecular Formula]
C21H18ClFN6O2 | [MDL Number]
MFCD28143918 | [MOL File]
1453848-26-4.mol | [Molecular Weight]
440.86 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Description]
GDC-0994 is a potent and selective ERK1 and ERK2 inhibitor with IC50 values of 6.1 and 4.1 nM, respectively.1 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.1 | [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. |
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