724440-27-1

724440-27-1 structure

Name: BAY 8002
Chemical Name: BAY-8002
CAS Number: 724440-27-1
Molecular Formula: C₂₀H₁₄ClNO₅S
Molecular Weight: 415.85
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Monocarboxylate Transporter
Create Date: 2019-06-03 12:42:23
Modify Date: 2024-01-07 22:58:19
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].

Name	BAY-8002

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.