Description
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 . 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 . 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 .
Product information
CAS Number: 15639-50-6
Molecular Weight: 301.51
Formula: C18H39NO2
Chemical Name: (2S,3S)-2-aminooctadecane-1,3-diol
Smiles: CCCCCCCCCCCCCCC[C@H](O)[C@@H](N)CO
InChiKey: OTKJDMGTUTTYMP-ROUUACIJSA-N
InChi: InChI=1S/C18H39NO2/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-18(21)17(19)16-20/h17-18,20-21H,2-16,19H2,1H3/t17-,18-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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