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SLV-2436
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SLV-2436图片
CAS NO:2095704-43-9
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
SEL201-88
SEL-201
产品介绍
SLV-2436 是一种高效且 ATP 竞争性的MNK1MNK2抑制剂,IC50分别为 10.8 nM 和 5.4 nM。
生物活性

SLV-2436 is a highly potent and ATP-competitive inhibitor ofMNK1andMNK2withIC50s of 10.8 nM and 5.4 nM, respectively.

IC50& Target

MNK2

5.4 nM (IC50)

MNK1

10.8 nM (IC50)

体外研究
(In Vitro)

To confirm the kinome selectivity of SLV-2436 (SEL201), the broad KINOMEscan competitive binding assay is performed at 1 μM, which includes 450 distinct kinases. The observed binding profile for SLV-2436 is significantly concentrated in the CAMK family of kinases that comprises MNK1 and MNK2. SLV-2436-treatedKIT-mutant melanoma cells have lower oncogenicity and reduced metastatic ability[1].

体内研究
(In Vivo)

To investigate the pharmacodynamic properties of SLV-2436 (SEL201), 5 consecutive oral doses of 10, 25, and 50 mg/kg are administered to mice every 12 hours (twice-daily schedule). At the 10 mg/kg twice-daily dosage, 4 hours after the fifth administration, a low plasma concentration of 125 ng/mL SLV-2436 is determined. However, dosing at 25 and 50 mg/kg twice daily, equivalent to 50 and 100 mg/kg/d of SLV-2436, yields 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, SLV-2436 is 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 SLV-2436 at the dosage of 50 mg/kg twice daily, that is, 100 mg/kg/d, for 37 days is well tolerated in mice[1].

分子量

350.80

性状

Solid

Formula

C19H15ClN4O

CAS 号

2095704-43-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL(285.06 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.8506 mL14.2531 mL28.5063 mL
5 mM0.5701 mL2.8506 mL5.7013 mL
10 mM0.2851 mL1.4253 mL2.8506 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。