产品说明书

ABC294640

Print
Chemical Structure| 915385-81-8 同义名 : Opaganib
CAS号 : 915385-81-8
货号 : A110039
分子式 : C23H25ClN2O
纯度 : 99%+
分子量 : 380.91
MDL号 : MFCD22666355
存储条件:

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:

2% DMSO+30% PEG 300+5% Tween 80+water 5 mg/mL

生物活性
描述 Sphingosine is an intermediate of sphingolipids that can be rapidly phosphorylated by sphingosine kinase (SK1 and SK2) to produce sphingosine 1-phosphate, which is a mitogenic compound. ABC294640 is a selective inhibitor of SK2 with a Ki value of 9.8 μM. ABC294640 dose-dependently inhibited recombinant human SK2 with an IC50 value of 60μM, while the activity of SK1 was not affected by ABC294640 at the concentration up to 100μM. In MDA-MB-231 cells, ABC294640 decreased [3H]S1P formation in a dose-dependent manner with an IC50 value of 26μM. ABC294640 also inhibited the proliferation of human tumor cell lines (1025LU, A-498, Caco-2, HT-29, DU145, SK-OV-3) with IC50 values ranging from 10.5-48.1μM[2]. In a mouse model of tri-nitrobenzene sulfonic acid (TNBS)-induced colitis, oral administration of ABC294640 (50mg/kg, twice daily) decreased TNBS-induced increase in mucosal myeloperoxidase activity by 60%. The histological analysis on colon sections revealed that the inflammation and damage caused by TNBS was reduced or negated by ABC294640 treatment[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.13mL

2.63mL

1.31mL

26.25mL

5.25mL

2.63mL

参考文献

[3]Maines LW, Fitzpatrick LR, Green CL, Zhuang Y, Smith CD. Efficacy of a novel sphingosine kinase inhibitor in experimental Crohn's disease. Inflammopharmacology. 2010 Apr;18(2):73-85. doi: 10.1007/s10787-010-0032-x. Epub 2010 Feb 12. PMID: 20151210.