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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Monocarboxylate Transporter (MCT)-BAY-8002
BAY-8002

Chemical Structure : BAY-8002

CAS No.: 724440-27-1

BAY-8002 (BAY8002;BAY 8002)

货号: PC-35589Not For Human Use, Lab Use Only.

BAY-8002 is a novel potent, selective, orally available monocarboxylate transporter 1 (MCT1) inhibitor (Kd=7.9 nM), inhibits cellular lactate uptake in DLD-1 cells with IC50 of 8 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BAY-8002 is a novel potent, selective, orally available monocarboxylate transporter 1 (MCT1) inhibitor (Kd=7.9 nM), inhibits cellular lactate uptake in DLD-1 cells with IC50 of 8 nM.
BAY-8002 displays no significant activity against in MCT4 expressing cells.
BAY-8002 inhibits cellular SNARF-5 fluorescence change with an IC50 of 85 nM in MCT1-expressing DLD-1 cells and displays excellent selectivity against MCT4 (IC50 >50 uM in EVSA-T cells).
BAY-8002 inhibits lactate uptake in MCT2-expressing oocytes, with ~5-fold lower potency compared to the MCT1 isoform.
BAY-8002 significantly increases intratumor lactate levels and transiently modulates pyruvate levels, inhibits Raji (IC50=0.67 uM) but not WSU-DLCL2 tumor growth.

物理化学性质&存储条件

分子量 415.844
分子式 C20H14ClNO5S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(2-chloro-5-(phenylsulfonyl)benzamido)benzoic acid

参考文献

1. Quanz M, et al. Mol Cancer Ther. 2018 Aug 16. pii: molcanther.1253.2017.

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