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Chemical Structure| 2095704-43-9 同义名 : SEL-201;SEL201-88
CAS号 : 2095704-43-9
货号 : A781993
分子式 : C19H15ClN4O
纯度 : 99%+
分子量 : 350.802
MDL号 : MFCD31728203
存储条件：

Pure form Keep in dark place,Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(299.31 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.29mL

14.25mL

2.85mL

1.43mL

28.51mL

5.70mL

2.85mL
参考文献

[1]Zhan Y, Guo J, et al. MNK1/2 inhibition limits oncogenicity and metastasis of KIT-mutant melanoma. J Clin Invest. 2017 Nov 1;127(11):4179-4192.