Ravoxertinib (GDC-0994) - Moligand™, 10mM in DMSO , MAP kinase ERK2 inhibitor, CAS No.1453848-26-4, MAP kinase ERK2 inhibitor

CAS: 1453848-26-4 Cat. No.: R408559 Molecular Weight: 440.86 PubChem CID: 71727581

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

(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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

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

GDC-0994 potently inhibits phospho-p90RSK in tumor cells.

In vivo

GDC-0994 (p.o.) results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice. In vivo, GDC-0994 (p.o.) inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways, and subsequently prevents ERK-dependent tumor cell proliferation and survival.
Cell Data

cell lines：MM cells, including INA6, RPMI-8226, U266, and RPMI-Dox40

Concentrations：

Incubation Time：

Powder Purity:≥98%

Specifications

Synonyms

(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

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

MAP kinase ERK2 inhibitor

Product Properties

• ALogP: 2

Names and Identifiers

• 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
• PubChem CID: 71727581
• Molecular Weight: 440.86

Associated Targets(Human)

Tchem Uncharacterized protein FLJ45252 (1 Activities)

Explore this target

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 (7 Activities)

Discover Target: MAPK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPK3 Tchem Mitogen-activated protein kinase 3 (3 Activities)

Discover Target: MAPK3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)