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KWR137

Chemical Structure : KWR137

CAS No.:

KWR137 (KWR-137)

Catalog No.: PC-24057Not For Human Use, Lab Use Only.

KWR137 is a novel potent inhibitor of Werner protein WRN with IC50 of 8 nM (WRN ATPase).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

KWR137 is a novel potent inhibitor of Werner protein WRN with IC50 of 8 nM (WRN ATPase).
KWR137 is more potent than HRO761 on WRN ATPase activity, but slightly weaker effect on WNR helicase activity.
KWR137 exhibits a GI50 value of 0.352 μM in SW48 cells.
KWR137 induces WRN degradation in the MSI-H CRC cells, SW48 and HCT116, but caused no degradation in the MSS CRC cell line, SW620. KWR137 (40 mg/kg, oral, daily) exhibits significant antitumor effects in SW48 cell xenograft model mice.

Physicochemical Properties

M.Wt 710.12
Formula C33H31ClF3N9O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(6-(4-(1H-pyrrolo[3,2-b]pyridine-2-carbonyl)piperazin-1-yl)-2-(3,6-dihydro-2H-pyran-4-yl)-5-ethyl-7-oxo-[1,2,4]triazolo[1,5-a]pyrimidin-4(7H)-yl)-N-(2-chloro-4-(trifluoromethyl)phenyl)acetamide

References

1. Moon B, et al. Bioorg Med Chem Lett. 2025 Feb 14:130141.

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