| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S88568-1mg买3赠1 |
99.00% | ￥550.00 |
5 | - | - | - | - |
|
S88568-5mg促销 |
99.00% | ￥1360.00 ￥1080.00 |
6 | - | - | - | - |
|
S88568-10mg促销 |
99.00% | ￥2240.00 ￥1790.00 |
6 | - | - | - | - |
|
S88568-25mg促销 |
99.00% | ￥3720.00 ￥2970.00 |
5 | - | - | - | - |
|
S88568-50mg促销 |
≥98% | ￥5700.00 ￥4560.00 |
货期：2-3天 | - | - | - | - |
|
S88568-100mg促销 |
≥98% | ￥7800.00 ￥6240.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | 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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| 靶点： | MNK2:5.4 nM (IC50);MNK1:10.8 nM (IC50);MNK | ||||||||||||||||||||
| 体外研究： | 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-treated KIT-mutant melanoma cells have lower oncogenicity and reduced metastatic ability | ||||||||||||||||||||
| 体内研究： | 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 | ||||||||||||||||||||
| 参考文献： | 1. Zhan Y, et al. MNK1/2 inhibition limits oncogenicity and metastasis of KIT-mutant melanoma. J Clin Invest. 2017 Nov 1;127(11):4179-4192. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20°C | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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