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ABC294640

In stock
Catalog No.
B1182
Sphingosine kinase 2 inhibitor,selective and competitive
Grouped product items
SizePriceStock Qty
5mg
$85.00
In stock
25mg
$279.00
In stock
100mg
$685.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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ABC294640 is a selective and competitive inhibitor of sphingosine kinase 2 (SK2) with IC50 value of 60μM [1].

ABC294640 is a competitive inhibitor of SK2. It shows IC50 value of about 60μM against recombinant human SK2. In the kinetic assay, ABC294640 competes with sphingosine and exerts a Ki value of 9.8μM. Because of its targeting of the sphingosine binding site of SK2, ABC294640 shows no inhibition activity against other 20 kinases. In MDA-MB-231 cells, ABC294640 prevents S1P production with IC50 value of 26μM. Moreover, ABC294640 has anti-proliferation and anti-migration efficacies in tumor cells. It suppresses cell proliferation of a variety of tumor cell lines such as 1025LU, A-498, Caco-2 and HT-29. The IC50 values are ranged from 6μM to 48μM. Furthermore, administration of ABC294640 inhibits tumor growth in the immunocompetent BALB/c mice bearing mammary adenocarcimona xenografts. Besides that, ABC294640 is also found to have greater anti-proliferation effects in ER-positive than ER-negative breast cancer cells. The effect of E2 signaling caused by ABC294640 is expected to be a therapeutic in endocrine-related diseases [1, 2].

References:
[1] French K J, Zhuang Y, Maines L W, et al. Pharmacology and antitumor activity of ABC294640, a selective inhibitor of sphingosine kinase-2. Journal of Pharmacology and Experimental Therapeutics, 2010, 333(1): 129-139.
[2] Antoon J W, White M D, Meacham W D, et al. Antiestrogenic effects of the novel sphingosine kinase-2 inhibitor ABC294640. Endocrinology, 2010, 151(11): 5124-5135.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt380.91
Cas No.915385-81-8
FormulaC23H25ClN2O
Solubility≥38.1mg/mL in DMSO
Chemical Name(7S)-3-(4-chlorophenyl)-N-(pyridin-4-ylmethyl)adamantane-1-carboxamide
SDFDownload SDF
Canonical SMILESC1C2CC3(CC1CC(C2)(C3)C(=O)NCC4=CC=NC=C4)C5=CC=C(C=C5)Cl
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.

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