Selumetinib (AZD6244) - Moligand™, 10mM in DMSO , Dual specificity mitogen-activated protein kinase kinase 2 inhibitor, CAS No.606143-52-6, Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

CAS: 606143-52-6 Cat. No.: S407860 Peso molecular: 457.69 Número EC: 641-434-6 PubChem CID: 10127622

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

ARRY-142886

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

In vitro

AZD6244 is not competitive with ATP and inactivates the ERK1/2 phosphorylation with IC50 concentrations below 40 nM. AZD6244 also inhibits the growth of primary HCC cells through inhibition of ERK1/2 and p90^RSK phosphorylation, accompanied with elevation of the cleavage of caspase-3 and caspase-7, and cleaved poly(ADP)ribose polymerase. AZD6244 has little effects on the p38, c-Jun-NH₂-kinase, phosphatidylinositol 3-kinase, and MEK5/ERK5 pathways. AZD6244 is sensitive to Raf mutations in breast cancer cell lines and Ras mutations in NSCLC cell lines.

In vivo

AZD6244 significantly inhibits phosphorylation of ERK1/2 in 2-1318, 5-1318, 26-1004 and 4-1318 xenografts and induces apoptosis in primary 2-1318 cells by activating the caspase pathway. AZD6244 could inhibit the tumor growth in HT-29 xenograft, which is a colorectal tumor model carrying a B-Raf mutation, at a dose of 100 mg/kg and the tumor growth inhibition of AZD6244 is better than it of Gemcitabine. Otherwise AZD6244 could inhibit HCC xenografts tumor growth, which associated with increased apoptosis and down-regulation of cell cycle regulators, including cyclin D1, Cdc-2, CDK2 and 4, cyclin B1, and c-Myc.
Cell Data

cell lines：

Concentrations：~ 10 μM

Incubation Time：24 or 48 hours

Powder Purity:≥99%

Specifications

Sinónimos

ARRY-142886

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Selumetinib (AZD6244, ARRY-142886) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf,

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

ALLOSTERIC MODULATOR, INHIBITOR

Mecanismo de acción

Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

Propiedades del producto

• ALogP: 3.6

Nombres e identificadores

• Isómeros SMILES: CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO
• PubChem CID: 10127622
• Peso molecular: 457.69

Objetivos asociados (humanos)

SMC2 Tchem Structural maintenance of chromosomes protein 2 (1 Activities)

Discover Target: SMC2

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

SMC1A Tchem Structural maintenance of chromosomes protein 1A (1 Activities)

Discover Target: SMC1A

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

Tchem Uncharacterized protein FLJ45252 (1 Activities)

Explore this target

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

MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 (2 Activities)

Discover Target: MAP2K1

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

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 49 mg/mL (200.58 mM); Water: Insoluble; Ethanol: Insoluble

Referencias

1. Song Xiaoping, Wang Lina, Tang Wei, Yuan Luyao, Liu Qingchao, Li Jing, Fan Daidi.  (2023)  Selumetinib overcomes gefitinib primary and acquired resistance by regulating MIG6/STAT3 in NSCLC.  ARCHIVES OF PHARMACAL RESEARCH,      [PMID:38032449] [10.1007/s12272-023-01471-0]