HRO761 | WRN inhibitor | Probechem Biochemicals

Chemical Structure : HRO761

CAS No.: 2869954-34-5

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

货号: 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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5 mg	￥880	In stock
10 mg	￥1280	In stock
25 mg	￥2180	In stock
50 mg	￥3580	In stock
100 mg	￥5580	In stock
250 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	702.09
分子式	C31H31ClF3N9O5
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	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

参考文献

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

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

生物&药学活性

物理化学性质&存储条件

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

生物&药学活性

物理化学性质&存储条件

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