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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-P-glycoprotein (P-gp)-WS-917
WS-917

Chemical Structure : WS-917

CAS No.:

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WS-917 (WS917)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 355.43
分子式 C16H13N5OS2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

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

参考文献

1. Shuai Wang, et al. J Med Chem. 2024 Oct 19. doi: 10.1021/acs.jmedchem.4c01081.

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