[CAS NO. 915385-81-8] Opaganib (ABC294640)

Name: Opaganib (ABC294640)
Brand: Arctom Scientific
SKU: SLK-S7174

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PRODUCTS SPECIFICATIONS [915385-81-8]

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Catalog

SLK-S7174

Brand

Selleck

CAS

915385-81-8

DESCRIPTION [915385-81-8]

Overview

MDL	MFCD22666355
Molecular Weight	380.91
Molecular Formula	C23H25ClN2O
SMILES	C(NCC=1C=CN=CC1)(=O)C23CC4(CC(C2)CC(C4)C3)C5=CC=C(Cl)C=C5

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.6253 mL	13.1265 mL	26.2529 mL
5 mM	0.5251 mL	2.6253 mL	5.2506 mL
10 mM	0.2625 mL	1.3126 mL	2.6253 mL
50 mM	0.0525 mL	0.2625 mL	0.5251 mL

Description

Opaganib (ABC294640) is an orally bioavailable and selective inhibitor with of approximately 60 μM. Phase 1/2.

Targets

SphK2 ^[1]
(Cell-free assay)

60 μM

In vitro

ABC294640 markedly alters the ratio of ceramide/S1P consistent with inhibition of SK activity in MDA-MB-231 cells. ABC294640 inhibits tumor cell proliferation with IC50 values ranging from approximately 6 to 48 μM, and impairs tumor cell migration concomitant with loss of microfilaments. ABC294640 induces nonapoptotic cell death, morphological changes in lysosomes, formation of autophagosomes, and increases in acidic vesicles in A-498, PC-3, and MDA-MB-231 cells. In both MCF-7 and ER-transfected HEK293 cells, ABC294640 decreases E2-stimulated ERE-luciferase activity.

In vivo

In mice bearing mammary adenocarcinoma xenografts, ABC294640 (100 mg/kg, p.o.) significantly reduce tumor growth, associated with depletion of S1P levels. In severe combined immunodeficient mice bearing A-498 xenografts, ABC294640 delays tumor growth and elevates autophagy markers. ABC294640 protects against liver transplantation-induced inflammation and cross-talk between innate and adaptive immunities, major events precipitating and exacerbating graft injury, and improves liver function and survival.

References

[1] French KJ, et al. J Pharmacol Exp Ther. 2010, 333(1), 129-139.
[2] Beljanski V, et al. J Pharmacol Exp Ther. 2010, 333(2), 454-464.
[3] Antoon JW, et al. Endocrinology. 2010, 151(11), 5124-5135.
[4] Liu Q, et al. PLoS One. 2012, 7(7), e41834.

Synonyms

Tricyclo[3.3.1.1^3,7]decane-1-carboxamide, 3-(4-chlorophenyl)-N-(4-pyridinylmethyl)-

3-(4-Chlorophenyl)-N-(4-pyridinylmethyl)tricyclo[3.3.1.1^3,7]decane-1-carboxamide

ABC 294640

Opaganib