产品
编 号：F752795
分子式：C26H20ClN3O6S
分子量：537.97
分子式：C26H20ClN3O6S
分子量：537.97
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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询价
结构图
CAS No: 2445185-57-7
产品详情
生物活性：
MSC-4381 (MCT4-IN-1) is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki 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. MSC-4381 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
MSC-4381 (化合物 18n；30 mg/kg；口服单剂量) 仅与 MCT1/2 抑制剂联合使用时表现出显著的肿瘤细胞内乳酸积累。 MSC-4381 (30 mg/kg/天；持续 15 天) 未显示出显著的抗肿瘤活性。 MSC-4381 (0.2 mg/kg；iv) 的 T1/2 为 1 小时，CL 为 0.33 L/h kg，Cmax 为 489 ng/mL，小鼠的 Vss 为 0.4 L/kg。Animal Model:MC38 tumor-bearing C57/BL6 mice
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
Dosage:0.2 mg/kg (Pharmacokinetic Analysis)
Administration:IV
Result:Had a T1/2 of 1 hours, a CL of 0.33 L/h?kg, a Cmax of 489 ng/mL and a Vss of 0.4 L/kg for mice.
体外研究：
MSC-4381 (化合物 18n) 抑制 MDA-MB-231 细胞系中的乳酸流出，IC50 为 1 nM。通过荧光互相关光谱 (FCCS) 确认了靶向活性，Ki 为 11 nM。 MSC-4381 在 SNU-398 和 MiaPaca2 中对乳酸流出的抑制程度相似，在 RT-4 细胞系中仅低 600 倍。
MSC-4381 (MCT4-IN-1) is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki 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. MSC-4381 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
MSC-4381 (化合物 18n；30 mg/kg；口服单剂量) 仅与 MCT1/2 抑制剂联合使用时表现出显著的肿瘤细胞内乳酸积累。 MSC-4381 (30 mg/kg/天；持续 15 天) 未显示出显著的抗肿瘤活性。 MSC-4381 (0.2 mg/kg；iv) 的 T1/2 为 1 小时，CL 为 0.33 L/h kg，Cmax 为 489 ng/mL，小鼠的 Vss 为 0.4 L/kg。Animal Model:MC38 tumor-bearing C57/BL6 mice
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
Dosage:0.2 mg/kg (Pharmacokinetic Analysis)
Administration:IV
Result:Had a T1/2 of 1 hours, a CL of 0.33 L/h?kg, a Cmax of 489 ng/mL and a Vss of 0.4 L/kg for mice.
体外研究：
MSC-4381 (化合物 18n) 抑制 MDA-MB-231 细胞系中的乳酸流出，IC50 为 1 nM。通过荧光互相关光谱 (FCCS) 确认了靶向活性，Ki 为 11 nM。 MSC-4381 在 SNU-398 和 MiaPaca2 中对乳酸流出的抑制程度相似，在 RT-4 细胞系中仅低 600 倍。
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