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Safingol

In stock
Catalog No.
C3243
PKC and sphingosine kinases inhibitor
Grouped product items
SizePriceStock Qty
1mg
$83.00
In stock
5mg
$269.00
In stock
10mg
$497.00
In stock

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Email: [email protected]

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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[[email protected]](N)[[email protected]@H](O)CCCCCCCCCCCCCCC
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

Safingol