Selective, non-ATP competitive inhibitor of sphingosine kinase (IC50 = 0.5µM GST-hSK; IC50 = 1.1µM intact JC mouse mammary adenovirus carcinoma cells) showing no inhibition of hERK2, hPI3k and hPKCα at concentrations up to 60µM. Cytotoxic effects have been demonstrated against various tumor cell lines including some overexpressing P-glycoprotein or MRP1 (T24, IC50 = 4.6µM; MCF-7, IC50 = 1.2µM; NCI/ADR, IC50 = 1.3µM, MCRF-7/VP, IC50 = 0.9µM). Induced apoptosis in T24 tumor cells.
Product Details
| Alternative Name: | 4-[[4-(4-Chlorophenyl)-1,3-thiazol-2-yl]amino]phenol |
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| Formula: | C15H11ClN2OS |
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| MW: | 302.8 |
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| Source: | Synthetic. |
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| CAS: | 312636-16-1 |
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| Purity: | ≥98% (TLC) |
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| Appearance: | Off-white solid. |
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| Solubility: | Soluble in DMSO (>25mg/ml) or 100% ethanol (>25mg/ml). |
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| Shipping: | Blue Ice |
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| Long Term Storage: | -20°C |
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| Handling: | Protect from light and air. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Antitumor Activity of Sphingosine Kinase Inhibitors: K.J. French, et al.; J. Pharmacol. Exp. Ther.
318, 596 (2006),
Abstract;
Full Text
Discovery and Evaluation of Inhibitors of Human Sphingosine Kinase: K.J. French, et al.; Cancer Res.
63, 5962 (2003),
Abstract;
Full Text
