首页 MAPK MNK SLV2436
SLV2436
编号 T4424     别名: SLV 2436, SLV-2436, SEL-201, SEL201-88, SLV-2436, SLV 2436, SEL201-88 SEL-201
CAS 2095704-43-9     分子式 C19H14ClN4O     分子量 349.79
靶点: MNK1; MNK2;
SLV-2436 (SEL201) is a novel effective and ATP-competitive inhibitor of MNK1 and MNK2 (IC50: 10.8/5.4 nM).
选择批次  
规格 库存 单价 数量
1 mg 上海现货 721.00
2 mg 上海现货 1082.00
5 mg 上海现货 1947.00
10 mg 上海现货 3117.00
25 mg 上海现货 6546.00
50 mg 上海现货 9867.00
100 mg 上海现货 14367.00
1 mL * 10 mM (in DMSO) 上海现货 1947.00
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生物活性

产品描述

SLV-2436 (SEL201) is a novel effective and ATP-competitive inhibitor of MNK1 and MNK2 (IC50: 10.8/5.4 nM).

靶点活性

MNK1,

MNK2,

体外活性

In vitro kinase assays, using recombinant MNK1 and MNK2 protein and increasing concentrations of the SEL201 show that SEL201 is highly potent, with an IC50 of 10.8  nM and 5.4  nM for MNK1 and MNK2, respectively. To confirm the kinome selectivity of SEL201, the broad KINOMEscan (DiscoverX) competitive binding assay at 1 μM is performed, which included 450 distinct kinases (32). The binding profile for SEL201 is observed, which was significantly concentrated in the CAMK family of kinases that comprises MNK1 and MNK2.

体内活性

To investigate the pharmacodynamic properties of SEL201, 5 consecutive oral doses of 10, 25, and 50 mg/kg were administered to mice every 12 hours (twice-daily schedule). At the 10 mg/kg twice-daily dosage, 4 hours after the fifth administration, we determined a low plasma concentration of 125 ng/ml SEL201. However, dosing at 25 and 50 mg/kg twice daily, equivalent to 50 and 100 mg/kg/d of SEL201, yielded substantially increased dose-dependent plasma exposure, reaching an average level of 1,299 ng/ml and 2,075 ng/ml, respectively. At the 24-hour time point, SEL201 was still detectable in the plasma, with dose-dependent concentrations of 9, 73, and 124 ng/ml in the 10, 25, and 50 mg/kg twice-daily treatment groups. Oral (p.o.) administration of SEL201 at the dosage of 50 mg/kg twice daily, that is, 100 mg/kg/d, for 37 days was well tolerated in mice. Furthermore, 37 days of consecutive administration of SEL201, at the dosage of 100 mg/kg/d, did not result in any overt clinical signs of toxicity. A blood chemistry panel was performed, including hematological and biochemical parameters, at the study endpoint and confirmed that multiple dosings with SEL201 at 100 mg/kg/d is safe. Nevertheless, SEL201 showed very good oral bioavailability, with a maximum plasma concentration of 1,078 ng/ml reached 0.25 hours after p.o. administration.

化学信息

分子量

349.79

分子式

C19H14ClN4O

CAS

2095704-43-9

溶解度

DMSO: 10 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.859 ml 14.294 ml 28.589 ml
5 mM 0.572 ml 2.859 ml 5.718 ml
10 mM 0.286 ml 1.429 ml 2.859 ml
50 mM 0.057 ml 0.286 ml 0.572 ml
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  • 经典已知活性库
  • 抗癌化合物库
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