Ravoxertinib (GDC-0994) is a potent, orally available, selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.

 

Brand: BCM

 

Target: ERK

 

Signaling Pathways: MAPK

 

In Vitro: GDC-0994 effectively inhibited phosphoric acid -p90RSK in tumor cells.

 

In Vivo: GDC-0994(oral) caused significant multiple single-dose activity in in vitro cancer models, including mice with KRAS mutant and BRAF mutant human xenografted tumors. In vivo, GDC-0994 (orally) inhibits ERK phosphorylation and activation of ERK-mediated signal transduction pathways, subsequently preventing ERK-dependent tumor cell proliferation and survival.

 

Boiling Point: 734.6±70.0 °C at 760 mmHg

 

Flash Point: 398.0±35.7 °C

 

pKa: 14.03±0.10(Predicted)

 

Solubility: Soluble in DMSO; soluble in Ethanol. Insoluble in Water. 

 

GHS: GHS07

 

Isomeric SMILES: CN1C(=CC=N1)NC2=NC=CC(=N2)C3=CC(=O)N(C=C3)[C@H](CO)C4=CC(=C(C=C4)Cl)F  

 

InChIKey: RZUOCXOYPYGSKL-GOSISDBHSA-N  

 

InChI: 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

 

Attribute
[Chem Name]	1-[(1S)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]pyridin-2-one
[Synonym]	Ravoxertinib; GDC-0994
[CAS No.]	1453848-26-4
[MDL No.]	MFCD28143918
[Formula]	C21H18ClFN6O2
[Molecular]	440.86
[Form]	Solid Powder
[Storage]	Keep in dark place. Inert atmosphere. Room temperature

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