AZD3965 - Moligand™, 10mM in DMSO , Inhibitor of Monocarboxylate transporter 1;Inhibitor of Monocarboxylate transporter 2, CAS No.1448671-31-5, Inhibitor of Monocarboxylate transporter 1;Inhibitor of Monocarboxylate transporter 2

CAS: 1448671-31-5 Cat. No.: A409212 Peso molecular: 515.51 PubChem CID: 10369242

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Thieno[2,​3-​d]​pyrimidine-​2,​4(1H,​3H)​-​dione, 5-​[[(4S)​-​4-​hydroxy-​4-​methyl-​2-​isoxazolidinyl]​carbonyl]​-​3-​methyl-​1-​(1-​methylethyl)​-​6-​[[5-​methyl-​3-​(trifluoromethyl)​-​1H-​pyrazol-​4-​yl]​methyl]​-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

AZD3965 AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 ( MCT1 ) inhibitor with a binding affinity of 1.6 nM, 6-fold selective over MCT2. Phase 1.
In vitro

In lymphoma cell lines that preferentially express MCT1, AZD3965 potently inhibits lactate transport and cell growth. AZD3965 inhibits MCT1 activity in cells, and shows higher sensitivity in hypoxia. In H526, HGC27 cells and DMS114 cells, AZD3965 increases intracellular lactate and significantly reduces lactate uptake.

In vivo

In nonobese diabetic scid-γ mice bearing COR-L103 xenografts, AZD3965 (100 mg/kg, p.o.) reduces tumor growth and increased intratumor lactate. In mice bearing H526 tumors, AZD3965 (100 mg/kg, p.o.) causes increased lactate concentration, a reduction in growth and increased radiation sensitivity.
Cell Data

cell lines：APP-overexpressing HEK293.

Concentrations：

Incubation Time：

Powder Purity:≥98%

Specifications

Sinónimos

Thieno[2, ​3-​d]​pyrimidine-​2, ​4(1H, ​3H)​-​dione, 5-​[[(4S)​-​4-​hydroxy-​4-​methyl-​2-​isoxazolidinyl]​carbonyl]​-​3-​methyl-​1-​(1-​methylethyl)​-​6-​[[5-​methyl-​3-​(trifluoromethyl)​-​1H-​pyrazol-​4-​yl]​methyl]​-

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 (MCT1) inhibitor with a binding affinity of 1.6 nM, 6-fold selective over MCT2. Phase 1.

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

INHIBITOR

Mecanismo de acción

Inhibitor of Monocarboxylate transporter 1;Inhibitor of Monocarboxylate transporter 2

Propiedades del producto

• ALogP: 2.066
• Recuento HBD: 1
• Enlace rotable: 5

Nombres e identificadores

• Isómeros SMILES: CC1=C(C(=NN1)C(F)(F)F)CC2=C(C3=C(S2)N(C(=O)N(C3=O)C)C(C)C)C(=O)N4C[C@](CO4)(C)O
• PubChem CID: 10369242
• Peso molecular: 515.51

Objetivos asociados (humanos)

SLC16A1 Tchem Monocarboxylate transporter 1 (1 Activities)

Discover Target: SLC16A1

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

Propiedades químicas y físicas

• DMSO (mg/ml) Solubilidad máxima: 100
• DMSO (mM) Solubilidad máxima: 193.982658
• Agua (mg/ml) Solubilidad máxima: ＜1