切换导航

Safingol

现货
Catalog No.
C3243
PKC和鞘氨醇激酶抑制剂
组合的产品项目
规格价格库存 数量
1mg
¥ 845.00
Ship with 10-15 days
5mg
¥ 2,743.00
Ship with 10-15 days
10mg
¥ 5,070.00
Ship with 10-15 days

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

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.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt301.5
Cas No.15639-50-6
FormulaC18H39NO2
SynonymsL-threo-Dihydrosphingosine,L-threo-Sphinganine
Solubility≤0.25mg/ml in ethanol
Chemical Name(2S,3S)-2-amino1,3-octadecanediol
SDFDownload SDF
Canonical SMILESOC[C@H](N)[C@@H](O)CCCCCCCCCCCCCCC
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。

质量控制

质量控制和MSDS

批次:

化学结构

Safingol