SKI-178
目录号: PL11419 纯度: ≥98%
CAS No. :1259484-97-3
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中文名称
SKI-178
英文名称
SKI-178
英文别名
SKI-178;1H-Pyrazole-5-carboxylic acid, 3-(4-methoxyphenyl)-, 2-[1-(3,4-dimethoxyphenyl)ethylidene]hydrazide;SKI 178;N-[1-(3,4-dimethoxyphenyl)ethylideneamino]-3-(4-methoxyphenyl)-1H-pyrazole-5-carboxamide;N-[(Z)-1-(3,4-dimethoxyphenyl)ethylideneamino]-3-(4-methoxyphenyl)-1H-pyrazole-5-carboxamide
Cas No.
1259484-97-3
分子式
C21H22N4O4
分子量
394.42
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
SKI-178 是一种有效的鞘氨醇激酶-1 (SphK1) 和 SphK2 抑制剂。SKI-178 对药物敏感和多药耐药癌细胞系 (如MTR3、NCI-ADR 和 HL60/VCR) 的 IC50 浓度范围为 1.8 到 0.1 μM。SKI-178 以 CDK1 依赖性方式诱导人急性髓性白血病细胞凋亡。
生物活性
SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC 50 concentrations ranging from 1.8 to 0.1 μM in both drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.
性状
Solid
体外研究(In Vitro)
SKI-178 (5 μM; 24 hours)-induced apoptotic cell death correlates with prolonged Bcl-2 phosphorylation. has not independently confirmed the accuracy of these methods. They are for reference only.Apoptosis AnalysisCe
体内研究(In Vivo)
SKI-178 (20 mg/kg; retro-orbital injection under isoflurane anesthesia) inhibits leukemic progression in the MLL-AF9 model. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: MLL-AF9 mou
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Hengst JA, et al. SKI-178: A Multitargeted Inhibitor of Sphingosine Kinase and Microtubule Dynamics Demonstrating Therapeutic Efficacy in Acute Myeloid Leukemia Models. Cancer Transl Med. 2017;3(4):109-121.
[2]. Hengst JA, et al. Development of a sphingosine kinase 1 specific small-molecule inhibitor. Bioorg Med Chem Lett. 2010;20(24):7498-7502.
溶解度数据
In Vitro: DMSO : 50 mg/mL (126.77 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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