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CAS No.: 2095704-43-9

SLV-2436 Catalog No. CSN22507

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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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

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.
参考文献

动物研究
剂量	Mice: 20 mg/kg/d - 100 mg/kg/d^[1] (p.o.)
给药途径	p.o.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8506 mL
- 14.2531 mL
- 28.5061 mL
- 5 mM
- 0.5701 mL
- 2.8506 mL
- 5.7012 mL
- 10 mM
- 0.2851 mL
- 1.4253 mL
- 2.8506 mL

技术信息

CAS号

2095704-43-9

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H15ClN4O

运输

蓝冰

分子量

350.80

别名

SEL201-88;SEL-201

溶解度

DMSO	70.0 mg/mL (199.5 mM)
Water	Insoluble
Ethanol	5.0 mg/mL (14.3 mM)

动物实验配方

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SLV-2436 Catalog No. CSN22507

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