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.
Acecainide HCl, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide.
Sematilide (CK-1752) hydrochloride is a novel class III antiarrhythmic agent.
EBE-A22 is a derivative of PD 153035, has no effect on EGF-R TK but maintains a high cytotoxic profile.
NIH-12848 is a putative phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) inhibitor.
CHS-828 (GMX1778) is a potent and specific inhibitor of NAMPT with IC50 and Kd value of <25 nM and 120 nM, respectively.
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