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 分子式: C₂₁H₂₄F₃N₅O₅S 分子量: 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

概要

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

同義語

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]​-

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

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.

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

INHIBITOR

作用メカニズム

Inhibitor of Monocarboxylate transporter 1;Inhibitor of Monocarboxylate transporter 2

製品の性質

• ALogP: 2.066
• HBD数: 1
• 回転可能な結合: 5

名前と識別子

• 異性体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
• 分子量: 515.51

関連ターゲット（人間）

SLC16A1 Tchem Monocarboxylate transporter 1 (1 Activities)

Discover Target: SLC16A1

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

化学的性質と物理的性質

• DMSO（mg / mL） 最大溶解度: 100
• DMSO（mM） 最大溶解度: 193.982658
• 水（mg / mL） 最大溶解度: ＜1