lactate transport inhibitor Contrary to the reference MCT1 inhibitor AR-C155858, 7ACC unexpectedly inhibited lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters. 7ACC delayed the growth of cervix SiHa tumors, colorectal HCT116 tumors, and orthoptopic MCF-7 breast tumors. MCT target engagement was confirmed by the lack of activity of 7ACC on bladder UM-UC-3 carcinoma that does not express functional MCT. 7ACC also inhibited SiHa tumor relapse after treatment with cisplatin. Finally, we found that contrary to AR-C155858, 7ACC did not prevent the cell entry of the substrate-mimetic drug 3-bromopyruvate (3BP) through MCT1, and contributed to the inhibition of tumor relapse after 3BP treatment.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||32 mg/mL in DMSO|
Antitumor activity of 7-aminocarboxycoumarin derivatives, a new class of potent inhibitors of lactate influx but not efflux.
Draoui N, et al. Mol Cancer Ther. 2014 Jun;13(6):1410-8. PMID: 24672058.
NSC 23766 is an inhibitor of Rac GTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM in a cell-free assay; does not inhibit the closely related targets, Cdc42 or RhoA.
Budesonide is a GC steroid commonly used for the treatment of asthma and non-infectious rhinitis.
Brequinar is a potent inhibitor of dihydroorotate dehydrogenase, with potent activities against a broad spectrum of viruses.
Laropiprant is a potent, selective DP1 receptor antagonist with Ki value of 0.57 nM, and exhibits > 1,000 fold selectivity over DP2 receptor (Ki=0.75 μM).
Thiazolidinediones (TZDs) are peroxisome proliferator-activated receptor γ agonists that improve insulin-mediated glucose uptake and possess beneficial vasculoprotective actions.
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