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Chemical Structure : WS-917
Catalog No.: PC-23219Not For Human Use, Lab Use Only.
WS-917 is a highly potent and orally available ABCB1 (MDR1, P-glycoprotein (P-gp)) modulator, enhance ABCB1 ATPase activity, exhibits a significant contributor to heightened sensitization of human colorectal adenocarcinoma cells (SW620/Ad300) to paclitaxel (IC50=5 nM).
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WS-917 is a highly potent and orally available ABCB1 (MDR1, P-glycoprotein (P-gp)) modulator, enhance ABCB1 ATPase activity, exhibits a significant contributor to heightened sensitization of human colorectal adenocarcinoma cells (SW620/Ad300) to paclitaxel (IC50=5 nM).
WS-917 possesses the capability to selectively stabilize ABCB1 through direct binding to the protein.
WS-917 substantially augmented intracellular paclitaxel and [3H]-paclitaxel, concurrently mitigating the efflux of [3H]-paclitaxel in SW620/Ad300 through the inhibition of ABCB1 efflux.
WS-917 induced stimulation of ABCB1 ATPase activity while exhibiting negligible inhibitory effect against CYP3A4.
WS-917 enhances the sensitivity of SW620/Ad300 to paclitaxel, as well as the sensitivity of CT26/TAXOL to paclitaxel and PD-L1 inhibitor (Atezolizumab) in vivo.
| M.Wt | 355.43 | |
| Formula | C16H13N5OS2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Shuai Wang, et al. J Med Chem. 2024 Oct 19. doi: 10.1021/acs.jmedchem.4c01081.
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