MSC-4381 (MCT4-IN-1) 是一种口服有效的，选择性的单羧酸转运蛋白 4 (MCT4/SLC16A3) 抑制剂，IC50值为 77 nM，Ki值为 11 nM。MSC-4381 靶向与 MCT4 的胞质域。MSC-4381 导致高表达 MCT4 细胞中乳酸流出的抑制和细胞活力的降低。MSC-4381 具有用于 MCT4 转运蛋白研究的潜力。
| 生物活性 | MSC-4381 (MCT4-IN-1) is an orally active and selectivemonocarboxylate transporter4 (MCT4/SLC16A3) inhibitor with anIC50of 77 nM and aKiof 11 nM. MSC-4381 targets to the cytosolic domain ofMCT4. MSC-4381 results in lactate efflux inhibition and reduction of cellular viability inMCT4high expressing cells. MSC-4381 has the potential forMCT4transporter inhibition research[1]. |
| IC50& Target | MCT4 77 nM (IC50) | MCT4 11 nM (Ki) |
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体外研究
(In Vitro) | MSC-4381 (compound 18n) inhibits lactate efflux in the MDA-MB-231 cell line with an IC50of 1 nM. The on-target activity is confirmed with a Kiof 11 nM by fluorescence cross-correlation spectroscopy (FCCS)[1].
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[1].
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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[1].
MSC-4381 (30 mg/kg/day; for 15 days) shows no significant antitumor activity[1].
MSC-4381 (0.2 mg/kg; iv) has a T1/2of 1 hours, a CL of 0.33 L/hokg, a Cmaxof 489 ng/mL and a Vssof 0.4 L/kg for mice[1].
| Animal Model: | MC38 tumor-bearing C57/BL6 mice[1] | | Dosage: | 30 mg/kg | | Administration: | PO; single dose | | Result: | Only combined with MCT1/2 inhibitor exhibited a significant tumoral intracellular lactate accumulation. |
| Animal Model: | Mice[1] | | Dosage: | 0.2 mg/kg (Pharmacokinetic Analysis) | | Administration: | IV | | Result: | Had a T1/2of 1 hours, a CL of 0.33 L/hokg, a Cmaxof 489 ng/mL and a Vssof 0.4 L/kg for mice. |
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| 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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 83.33 mg/mL(154.90 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 1.8588 mL | 9.2942 mL | 18.5884 mL | | 5 mM | 0.3718 mL | 1.8588 mL | 3.7177 mL | | 10 mM | 0.1859 mL | 0.9294 mL | 1.8588 mL |
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