BAY 8002

Names

[ Name ]:
BAY 8002

Biological Activity

[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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Monocarboxylate Transporter

Research Areas >> Cancer

[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.

[References]

[1]. Quanz M, et al. Preclinical Efficacy of the Novel Monocarboxylate Transporter 1 Inhibitor BAY-8002 and Associated Markers of Resistance. Mol Cancer Ther. 2018 Nov;17(11):2285-2296.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₁₄ClNO₅S

[ Molecular Weight ]:
415.85

[ Storage condition ]:
2-8℃

Related Compounds

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