Chemical Structure : RP-3467
CAS No.:
3098615-15-4
RP-3467
(RP3467)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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534.54
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Formula
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C26H20F2N6O3S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Rosen EY, et al. medRxiv [Preprint]. 2026 Sep 22:2026.09.16.26363059.
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