Chemical Structure : WS-917
CAS No.:
WS-917
(WS917)
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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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355.43
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Formula
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C16H13N5OS2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-((Benzo[d]thiazol-2-ylmethyl)thio)-4,5,6,7-tetrahydro-8H-cyclopenta[d][1,2,4]triazolo[1,5-a]pyrimidin-8-one
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References
1. Shuai Wang, et al. J Med Chem. 2024 Oct 19. doi: 10.1021/acs.jmedchem.4c01081.
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