RP-3467 | Polθ inhibitor | Probechem Biochemicals

Chemical Structure : RP-3467

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RP-3467 (RP3467)

货号: PC-28440Not For Human Use, Lab Use Only.

RP-3467 is a potent, selective inhibitor of DNA polymerase theta (Polθ) helicase domain with EC50 of <0.25 nM, shows no discernible inhibitory activity against other DNA repair-related ATPases WRN, BLM, and FANCM.

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生物&药学活性

RP-3467 is a potent, selective inhibitor of DNA polymerase theta (Polθ) helicase domain with EC50 of <0.25 nM, shows no discernible inhibitory activity against other DNA repair-related ATPases WRN, BLM, and FANCM.
RP-3467 stabilized an ectopically expressed Polθ ATPase construct with EC50 of 5 nM in CETSA assay.
RP-3467 suppresses MMEJ repair events in HCT116 cells with IC50 of 3 nM.
RP-3467 disrupts MMEJ and mitotic DNA repair in HRD cells, induces synthetic lethality in HR-deficient cells and synergizes with PARP inhibition.
RP-3467 enhances the anti-tumor activity of PARP inhibitors in HRD xenograft and PDX models.

物理化学性质&存储条件

分子量	534.54
分子式	C26H20F2N6O3S
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''-(difluoromethyl)-N-(5-((1S,2S)-2-ethynylcyclopropyl)-1,3,4-thiadiazol-2-yl)-5''-methoxy-4-methyl-2-oxo-2H-[1,2':4',4''-terpyridine]-5'-carboxamide

参考文献

1. Rosen EY, et al. medRxiv [Preprint]. 2026 Sep 22:2026.09.16.26363059.

RP-3467 (RP3467)

生物&药学活性

物理化学性质&存储条件

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RP-3467 (RP3467)

生物&药学活性

物理化学性质&存储条件

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