BAY-8002|MCT1 inhibitor|cas 724440-27-1|DC Chemicals

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.

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.