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HRO761

Chemical Structure : HRO761

CAS No.: 2869954-34-5

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HRO761 (HRO-761, Werner syndrome RecQ helicase-IN-1)

Catalog No.: PC-20674Not For Human Use, Lab Use Only.

HRO761 (HRO-761) is the first potent and selective, allosteric inhibitor of RecQ DNA helicase WRN with IC50 of 50 nM, shows potent and selective anti-tumor activity in cancers with microsatellite instability.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

HRO761 (HRO-761) is the first potent and selective, allosteric inhibitor of RecQ DNA helicase WRN with IC50 of 50 nM, shows potent and selective anti-tumor activity in cancers with microsatellite instability.
HRO761 binds at the interface of the D1 and D2 helicase domains, locking WRN in an inactive conformation.
Pharmacological inhibition of WRN by HRO761 recapitulates the phenotype observed by WRN genetic suppression, leading to activation of the DNA damage response and inhibition of tumor cell growth selectively in microsatellite instability (MSI) but not in MSS cells.
HRO761 activates a p53-related response, anti-proliferative effects were observed in both p53 wild-type as well as p53 null or mutated tumor cells.
HRO761 treatment results in dose-dependent in vivo DNA damage induction and tumor growth inhibition in MSI cell- and patient-derived xenograft models.

Physicochemical Properties

M.Wt 702.09
Formula C31H31ClF3N9O5
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

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

References

1. Patent WO2022249060 (Example 42).
2. Ferretti S, et al. Nature. 2024 Apr 24. doi: 10.1038/s41586-024-07350-y.

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