货号:A781993 同义名: SEL-201;SEL201-88
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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产品名称 | MNK1 ↓ ↑ | MNK2 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
CGP 57380 |
++
MNK1, IC50: 2.2 μM |
99%+ | |||||||||||||||||
Tomivosertib |
+++
MNK1, IC50: 2.4 nM |
++++
MNK2, IC50: 1 nM |
99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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. |
Dose | Mice: 20 mg/kg/d - 100 mg/kg/d[1] (p.o.) |
Administration | p.o. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 2095704-43-9 |
分子式 | C19H15ClN4O |
分子量 | 350.802 |
别名 | SEL-201;SEL201-88 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,2-8°C |
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 |