货号	规格	价格	上海	北京	珠海	重庆	武汉
S89211-5mg买3赠1	99.90%	￥560.00 S89211-5mg ￥560.00 现货（买3赠1）	5 5	-	-	-	-
S89211-10mg买3赠1	99.90%	￥970.00 S89211-10mg ￥970.00 现货（买3赠1）	6 6	-	-	-	-
S89211-25mg促销	99.90%	￥1870.00 ￥1490.00 S89211-25mg ￥1490.00 现货	4 4	-	-	-	-
S89211-100mg促销	≥98%	￥4500.00 ￥3600.00 S89211-100mg ￥3600.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both agent sensitive and multi-agent 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

靶点：

SphK1; SphK2

体外研究：

SKI-178 (5 μM; 24 hours)-induced apoptotic cell death correlates with prolonged Bcl-2 phosphorylation. Apoptosis Analysis Cell Line: HL-60 cells Concentration: 5 μM Incubation Time: 24 hours Result: JNK activity (indicated by phosphorylation at Thr183/Tyr185) increased in a time-dependent manner starting as early as 2 hours continued to increase for at least 24 hours. There was a concomitant increase in apoptotic cell death indicated by the cleavage of caspase-7. Bcl-2 phosphorylation at Ser70 increased with time in response to SKI-178 treatment, reaching maximal levels at 8 hours, which was consistent with the timing of caspase-7 activation.

体内研究：

SKI-178 (20 mg/kg; retro-orbital injection under isoflurane anesthesia) inhibits leukemic progression in the MLL-AF9 model. Animal Model: MLL-AF9 mouse model (leukemic mice) Dosage: 20 mg/kg Administration: Retro-orbital injection under isoflurane anesthesia; three times per week for 1 and 3 weeks Result: White blood cell (WBC) counts decreased from their initial 104 cells/μL levels and continued to decline after 3 weeks of treatment until they reached normal levels (~4×103 cells/μL).

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. 3. Dick TE, et al. The apoptotic mechanism of action of the sphingosine kinase 1 selective inhibitor SKI-178 in human acute myeloid leukemia cell lines. J Pharmacol Exp Ther. 2015;352(3):494-508.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.535 ml	12.677 ml	25.355 ml
5 mM	0.507 ml	2.535 ml	5.071 ml
10 mM	0.254 ml	1.268 ml	2.535 ml
50 mM	0.051 ml	0.254 ml	0.507 ml

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。

参考文献

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