GDC-0994

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.Formal Name: 1-[(1S)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl]-2(1H)-pyridinone. CAS Number: 1453848-26-4. Synonyms: RG-7842. Molecular Formula: C21H18ClFN6O2. Formula Weight: 440.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/mL, DMSO: 30 mg/mL, DMSO:PBS (pH 7.2)(1:9): 0.10 mg/mL, Ethanol: 30 mg/mL. lambdamax: 220, 332 nm. SMILES: O=C(N([C@H](CO)C1=CC(F)=C(Cl)C=C1)C=C2)C=C2C3=NC(NC4=CC=NN4C)=NC=C3. InChi Code: InChI=1S/C21H18ClFN6O2/c1-28-19(5-8-25-28)27-21-24-7-4-17(26-21)13-6-9-29(20(31)11-13)18(12-30)14-2-3-15(22)16(23)10-14/h2-11,18,30H,12H2,1H3,(H,24,26,27)/t18-/m1/s1. InChi Key: RZUOCXOYPYGSKL-GOSISDBHSA-N.