MSC-4381 (MCT4-IN-1) is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC 50 of 77 nM and a K i of 11 nM. MSC-4381 targets to the cytosolic domain of MCT4. MSC-4381 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MSC-4381 has the potential for MCT4 transporter inhibition research.
性状
Solid
IC50 & Target[1][2]
MCT4 77 nM (IC50) MCT4 11 nM (Ki)
体外研究(In Vitro)
MSC-4381 (compound 18n) inhibits lactate efflux in the MDA-MB-231 cell line with an IC50 of 1 nM. The on-target activity is confirmed with a Ki of 11 nM by fluorescence cross-correlation spectroscopy (FCCS). MSC-4381 does not inhibit lactate efflux to a similar extent in SNU-398 and MiaPaca2, and only 600-fold less in RT-4 cell lines. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
MSC-4381 (compound 18n; 30 mg/kg; PO; single dose) only combined with MCT1/2 inhibitor exhibits a significant tumoral intracellular lactate accumulation.
MSC-4381 (30 mg/kg/day; for 15 days) shows no significant antitumor activity.
MSC-4381 (0.2 mg/kg; iv) has a T 1/2 of 1 hours, a CL of 0.33 L/h?kg, a C max of 489 ng/mL and a V ss of 0.4 L/kg for mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Timo Heinrich, et al. Discovery of 5-{2-[5-Chloro-2-(5-ethoxyquinoline-8-sulfonamido)phenyl]ethynyl}-4-methoxypyridine-2-carboxylic Acid, a Highly Selective in Vivo Useable Chemical Probe to Dissect MCT4 Biology. J Med Chem. 2021 Aug 26;64(16):11904-11933.
溶解度数据
In Vitro: DMSO : 83.33 mg/mL (154.90 mM; ultrasonic and warming and heat to 60°C)配制储备液