AZD8330 - Moligand™, 10mM in DMSO , Dual specificity mitogen-activated protein kinase kinase 2 inhibitor, CAS No.869357-68-6, Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

CAS: 869357-68-6 Cat. No.: A409124 Fórmula: C₁₆H₁₇FIN₃O₄ Peso molecular: 461.23 Número CE: 642-441-7

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

ARRY704 | 2-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

Information

AZD8330 (ARRY704) is a novel, selective, non-ATP competitiveMEK 1/2inhibitor withIC50of 7 nM. Phase 1.
In vitro

AZD8330 potently and strongly inhibits MEK 1/2. AZD8330 has no inhibitory activity against over 200 other kinases including at concentrations up to 10 μM. AZD8330 demonstrates sub-nanomolar potency in mechanistic (pERK) and low to sub-nanomolar potency in functional (proliferation) assays in MEK 1/2 inhibitor sensitive cell lines.

In vivo

In a Calu-6 rat xenograft pharmacokinetic/pharmacodynamic (PK/PD) model a single, 1.25 mg/kg oral dose of AZD8330 inhibits ERK phosphorylation by > 90% for between 4 and 8 hours. Doses as low as 0.4 mg/kg once daily are sufficient for > 80% tumor growth inhibition in the Calu-6 nude rat xenograft model. In the Calu-6 model, AZD8330 inhibits tumor growth in a dose-dependent fashion, at 0.3 mg/kg and 1.0 mg/kg once daily.
Cell Data

cell lines：

Concentrations：~10 μM

Incubation Time：1 hour

Powder Purity:≥99%

Specifications

Sinónimos

ARRY704 | 2-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide

Especificações e pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos e fisiológicos

AZD8330 (ARRY704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Grau

Moligand™

Tipo de ação

INHIBITOR

Mecanismo de ação

Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

Propriedades do produto

ALogP

2.2

Nomes e identificadores

SMILES isoméricas

CC1=CC(=C(N(C1=O)C)NC2=C(C=C(C=C2)I)F)C(=O)NOCCO

Peso molecular

461.23

Reaxy-Rn

14467135

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=14467135&ln=

Alvos associados (humanos)

MAP2K2 Tclin Dual specificity mitogen-activated protein kinase kinase 2 (1 Activities)

Discover Target: MAP2K2

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

MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 (1 Activities)

Discover Target: MAP2K1

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

Propriedades químicas e físicas

• Solubilidade: Solubility (25°C) In vitro DMSO: 0.01 mg/mL (0.04 mM); Water: Insoluble; Ethanol: Insoluble
• Índice de refração: 1.66