1. Membrane Transporter/Ion Channel
  2. Monocarboxylate Transporter
  3. BAY-8002

BAY-8002 

目录号: HY-122312 纯度: 98.10%
产品使用指南

BAY-8002 是一种有效、选择性、可口服的单羧酸转运蛋白第 1 亚型 (monocarboxylate transporter 1 (MCT1)) 抑制剂,在表达 MCT1 的 DLD-1 细胞中,IC50 值为 85 nM,对 MCT1 的选择性远高于 MCT4。具有抗肿瘤活性。

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BAY-8002 Chemical Structure

BAY-8002 Chemical Structure

CAS No. : 724440-27-1

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Size Price Stock Quantity
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥110 In-stock
5 mg ¥1000 In-stock
10 mg ¥1500 In-stock
50 mg ¥4500 In-stock
100 mg ¥7500 In-stock
200 mg   Get quote  
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Description

BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity[1].

IC50 & Target

IC50: 85 nM (MCT1, in DLD-1 cells)[1]

In Vitro

BAY-8002 is an inhibitor of MCT1, with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4 (IC50 >50 µM in EVSA-T cells)[1].

In Vivo

BAY-8002 (80 and 160 mg/kg, p.o., twice daily, for more than 26 days) significantly inhibits tumor growth in Raji tumor-bearing mice[1].

Animal Model: Female NOD SCID mice bearing Raji cells (7-10 weeks old)[1]
Dosage: 80 and 160 mg/kg
Administration: P.O. twice daily for more than 26 days
Result: Inhibited tumor growth with no obvious body weight loss, but showed no effect on tumor regression.
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (300.59 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4047 mL 12.0236 mL 24.0471 mL
5 mM 0.4809 mL 2.4047 mL 4.8094 mL
10 mM 0.2405 mL 1.2024 mL 2.4047 mL
*请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液。
In Vivo:
  • 1.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.00 mM); Clear solution

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.00 mM); Clear solution

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (5.00 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在 MCE 网站选购。
References
Molecular Weight

415.85

Formula

C₂₀H₁₄ClNO₅S

CAS No.

724440-27-1

SMILES

O=C(O)C1=CC=CC=C1NC(C2=CC(S(=O)(C3=CC=CC=C3)=O)=CC=C2Cl)=O

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 98.10%

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产品名称:
BAY-8002
目录号:
HY-122312
需求量:

BAY-8002

Cat. No.: HY-122312