|2-(2-氯-5-(苯基磺酰基)苯甲酰氨基)苯甲酸|CsnPharm

CAS No.: 724440-27-1

BAY-8002 Catalog No. CSN23771

Synonyms: BAY8002

BAY-8002 is a potent MCT Inhibitor with IC50 value of 8nM for inhibition of L-lactate uptake.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述MCT1 (monocarboxylate transporter 1/ SLC16A1) plays a central role in tumor cell energy homeostasis. BAY-8002 is a novel class of MCT1 inhibitor which can potently suppress bidirectional lactate transport with IC50 value of 8nM and EC50 value of 7nM for L-lactate uptake and lactate export in DLD-1 cells. Also, BAY-8002 inhibited lactate uptake in MCT2-expressing oocytes, with approximately 5-fold lower potency compared with the MCT1 isoform. For the accumulation of lactate in the cell supernatant was inhibited by BAY8002, the change of intracellular pH and decrease of extracellular acidification rate could be observed. This inhibition of lactate transport resulted an efficient proliferation inhibition of Raji and Daudi Burkitt lymphoma cells expressed MCT1. Oral administration of BAY8002 at dose of 80 and 160mg/kg twice daily led a significant inhibition of tumor growth and modulation of intratumor lactate in Raji tumor–bearing mice but not WSU-DLCL2.
动物研究
剂量
Mice: 80 mg/kg, 160 mg/kg^[1] (p.o., BID)

给药途径
p.o.

动物研究
剂量	Mice: 80 mg/kg, 160 mg/kg^[1] (p.o., BID)
给药途径	p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4047 mL
- 12.0237 mL
- 24.0473 mL
- 5 mM
- 0.4809 mL
- 2.4047 mL
- 4.8095 mL
- 10 mM
- 0.2405 mL
- 1.2024 mL
- 2.4047 mL

技术信息

CAS号

724440-27-1

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H14ClNO5S

运输

蓝冰

分子量

415.85

别名

BAY8002

溶解度

DMSO	83.0 mg/mL (199.6 mM)
Water	Insoluble
Ethanol	28.0 mg/mL (67.3 mM)

动物实验配方

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