BAY-8002

  Cat. No.:  DC11218   Featured
Chemical Structure
724440-27-1
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More than 5000 active chemicals with high quality for research!
Field of application
BAY-8002 is a novel potent, selective, orally available monocarboxylate transporter 1 (MCT1) inhibitor (Kd=7.9 nM).
Cas No.: 724440-27-1
Chemical Name: 2-[[5-(Benzenesulfonyl)-2-chlorobenzoyl]amino]benzoic acid
Synonyms: BAY8002;2-(2-chloro-5-(phenylsulfonyl)benzamido)benzoic acid;GTPL10405;2-[[5-(benzenesulfonyl)-2-chlorobenzoyl]amino]benzoic acid;BCP30742;BAY 8002;ZB1541;s8747;BAY 8002; BAY8002;2-[[2-Chloro-5-(phenylsulfonyl)benzoyl]amino]benzoic acid;BAY-8002
SMILES: ClC1C([H])=C([H])C(=C([H])C=1C(N([H])C1=C([H])C([H])=C([H])C([H])=C1C(=O)O[H])=O)S(C1C([H])=C([H])C([H])=C([H])C=1[H])(=O)=O
Formula: C20H14ClNO5S
M.Wt: 415.8469
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
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].
Target: IC50: 85 nM (MCT1, in DLD-1 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.
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].
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC72788 AZD0095 AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib.
DC11218 BAY-8002 BAY-8002 is a novel potent, selective, orally available monocarboxylate transporter 1 (MCT1) inhibitor (Kd=7.9 nM).
DC9263 AZD-3965 AZD3965 is a selective inhibitor of monocarboxylate transporter 1 (MCT1) with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM.
DC7876 7ACC2 7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells.
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