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 Molecular Weight: 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

Overview

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

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]​-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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.

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

Inhibitor of Monocarboxylate transporter 1;Inhibitor of Monocarboxylate transporter 2

Product Properties

• ALogP: 2.066
• HBD Count: 1
• Rotatable Bond: 5

Names and Identifiers

• Isomeric 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
• Molecular Weight: 515.51

Associated Targets(Human)

SLC16A1 Tchem Monocarboxylate transporter 1 (1 Activities)

Discover Target: SLC16A1

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

Chemical and Physical Properties

• DMSO(mg / mL) Max Solubility: 100
• DMSO(mM) Max Solubility: 193.982658
• Water(mg / mL) Max Solubility: ＜1