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SafingolPKC和鞘氨醇激酶抑制剂

Safingol

产品编号:C3243
ApexBio 的所有产品仅用作科研,我们不为任何个人用途提供产品和服务
规格 单价 库存 订购数量
1mg ¥845.00 10-15 工作日发货
5mg ¥2,743.00 10-15 工作日发货
10mg ¥5,070.00 10-15 工作日发货

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Sample solution is provided at 25 µL, 10mM.

质量控制

质量控制和MSDS

批次:

化学结构

Safingol

Safingol Dilution Calculator

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Safingol Molarity Calculator

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化学性质

CAS号 15639-50-6 SDF Download SDF
别名 L-threo-Dihydrosphingosine,L-threo-Sphinganine
化学名 (2S,3S)-2-amino1,3-octadecanediol
SMILES OC[C@H](N)[C@@H](O)CCCCCCCCCCCCCCC
分子式 C18H39NO2 分子量 301.5
溶解度 ≤0.25mg/ml in ethanol 储存条件 Store at -20°C
物理性状 A crystalline solid 运输条件 试用装:蓝冰运输。
其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议 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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

产品描述

Ki: SphK with a Ki of about 5 μmol/L

Safingol is a sphingosine and PKC kinases inhibitor.

Sphingosine 1-phosphate, a product of sphingosine kinases (SphK), mediates various biological processes including cell proliferation, differentiation, motility, and apoptosis. Protein kinase C (PKC), is a family of protein kinase enzymes involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues.

In vitro: Safingol was identified as a potent competitive inhibitor of SphK and had significant in-vitro anticancer activity. Safingol could increase the in-vitro antitumor effect of various chemotherapeutic agents including cisplatin, doxorubicin, and mitomycin C via enhancing chemotherapy induced apoptosis. It was also found that safingol alone induced cell death by autophagy. Safingol was also extensively studied as an inhibitor of PKC, although the Ki was higher than that for SphK [1].

In vivo: Previous studies found that although safingol showed limited single-agent activity in vivo, xenograft experiments had indicated that safingol could increase the antitumor activity of cisplatin without increasing toxicity [1].

Clinical trial: Previous clinical study showed that safingol could be safely administered in combination with cisplatin. As expected from preclinical data, the reversible dose-dependent hepatic toxicity was observed. Target inhibition was achieved with downregulation of S1P. The recommended phase II dose is S 840 mg/m2 and C 60 mg/m2, every 3 weeks [1].

Reference:
[1] Dickson MA, Carvajal RD, Merrill AH Jr, Gonen M, Cane LM, Schwartz GK.  A phase I clinical trial of safingol in combination with cisplatin in advanced solid tumors. Clin Cancer Res. 2011 Apr 15;17(8):2484-92.