CAS:2095704-43-9SLV-2436

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Synonyms: SEL201-88;SEL-201

SLV-2436 is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50s of 10.8 nM and 5.4 nM, respectively.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

2095704-43-9

储存条件

分子式

C19H15ClN4O

运输

蓝冰

分子量

350.80

别名

SEL201-88;SEL-201

溶解度

动物实验配方

生物活性

描述SEL201 is an MNK1/2 inhibitor with IC50 values of 10.8nM and 5.4nM for MNK1 and MNK2, respectively, measured by recombinant MNK1/2 activity. SEL201 decreased KIT-mutant melanoma cells and reduced the metastatic ability. SEL201 potently suppressed MNK1/2 activity in our panel of KIT-mutant melanoma cell lines as determined by repressed phosphorylation of its substrate eIF4E. SEL201 at 5μM significantly decreased the colony-forming ability of both C-KIT D820Y and L576P mutant melanoma cell lines, but did not inhibit the proliferation of normal, nonmalignant MelST melanocytes. Oral administration of SEL201 at dose of 75mg/kg/day, 5 consecutive days per week, for 35 days significantly decreased both the number and the size of metastases in the lung in a xenograft model wherein KIT-mutant MM111 cells.
动物研究
剂量
Mice: 20 mg/kg/d - 100 mg/kg/d^[1] (p.o.)

给药途径
p.o.