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Opaganib

Opaganib (ABC294640) 是选择性和竞争性的鞘氨醇激酶 2 (SK2) 抑制剂，Ki 为 9.8 μM。

CAS号

915385-81-8

分子式

C23H25ClN2O

主要靶点

S1P Receptor

仅限科研使用

Cat No : CM06510

Print datasheet

Synonyms

ABC294640

验证数据展示

  • CAS No.: 915385-81-8

    Opaganib
    CAS#: 915385-81-8

产品信息

Opaganib (ABC294640) is an orally active and specific sphingosine kinase-2 (SphK2) inhibitor (IC50: 60 μM).

CAS号 915385-81-8
分子式 C23H25ClN2O
主要靶点 S1P Receptor
主要通路 G蛋白偶联受体
分子量 380.91
纯度 99.53%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 ABC294640

靶点活性

SphK2:60 μM

体内活性

In mice bearing mammary adenocarcinoma xenografts, ABC294640 (100 mg/kg, p.o.) significantly reduce tumor growth, associated with depletion of S1P levels. [1] In severe combined immunodeficient mice bearing A-498 xenografts, ABC294640 delays tumor growth and elevates autophagy markers. [2] 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. [4]

体外活性

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. [1] 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. [2] In both MCF-7 and ER-transfected HEK293 cells, ABC294640 decreases E2-stimulated ERE-luciferase activity. [3]

溶解度

Ethanol:27 mg/mL (70.9 mM),H2O:<1 mg/mL,DMSO:71 mg/mL (186.4 mM)

细胞实验

To determine the effects of the test compounds on proliferation, cells are plated into 96-well microtiter plates and allowed to attach for 24 h. Varying concentrations of ABC294640 are added to individual wells and the cells are incubated for an additional 72 h. At the end of this period, the number of viable cells is determined by use of the sulforhodamine-binding assay. The percentage of cells killed is calculated as the percentage decrease in sulforhodamine-binding compared with control cultures. Regression analyses of inhibition curves are performed by use of GraphPad Prism.(Only for Reference)

参考文献

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.

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The dilution calculator equation

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