Ulixertinib (BVD-523) - Moligand™, 10mM in DMSO , MAP kinase ERK2 inhibitor, CAS No.869886-67-9, MAP kinase ERK2 inhibitor

CAS: 869886-67-9 Cat. No.: U409233 Molecular Weight: 433.33 PubChem CID: 11719003

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

VRT752271 | 4-(5-chloro-2-(isopropylamino)pyridin-4-yl)-N-((S)-1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Ulixertinib (BVD-523) Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.
In vitro

In an A375 melanoma cell line containing a b-RAFV600E mutation, Ulixertinib reduces the levels of phosphorylated ERK2 (pERK) and of the phosphorylation of the downstream kinase RSK (pRSK) with IC50 of 4.1/0.14 μM, respectively. Ulixertinib also inhibits A375 cell proliferation with IC50 of 180 nM.

In vivo

Cell Data

cell lines：A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 cells

Concentrations：~30 μM

Incubation Time：72 h

Powder Purity:≥99%

Specifications

Synonyms

VRT752271 | 4-(5-chloro-2-(isopropylamino)pyridin-4-yl)-N-((S)-1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. 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: 4.266
• HBD Count: 4
• Rotatable Bond: 7

Names and Identifiers

• Isomeric SMILES: CC(C)NC1=NC=C(C(=C1)C2=CNC(=C2)C(=O)N[C@H](CO)C3=CC(=CC=C3)Cl)Cl
• PubChem CID: 11719003
• Molecular Weight: 433.33

Associated Targets(Human)

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

Discover Target: MAPK3

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

Chemical and Physical Properties

• DMSO(mg / mL) Max Solubility: 86
• DMSO(mM) Max Solubility: 198.4630651
• Water(mg / mL) Max Solubility: ＜1