MSC-4381
目录号: PL07524 纯度: ≥98%
CAS No. :2445185-57-7
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中文名称
MSC-4381
英文名称
MSC-4381
英文别名
2-​Pyridinecarboxylic acid, 5-​[2-​[5-​chloro-​2-​[[(5-​ethoxy-​8-​quinolinyl)​sulfonyl]​amino]​phenyl]​ethynyl]​-​4-​methoxy-;MSC-4381
Cas No.
2445185-57-7
分子式
C26H20ClN3O6S
分子量
537.97
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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 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
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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