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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-DNA/RNA Synthesis-RP-2119
RP-2119

Chemical Structure : RP-2119

CAS No.: 2922287-81-6

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RP-2119 (RP2119)

货号: PC-25495Not For Human Use, Lab Use Only.

RP-2119 (RP2119) is a selective, potent, and bioavailable inhibitor of DNA polymerase theta (Polθ) ATPase inhibitor with IC50 of 0.7 nM (hPOLθ ATPase) in ADP-glo assayss.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

RP-2119 (RP2119) is a selective, potent, and bioavailable inhibitor of DNA polymerase theta (Polθ) ATPase inhibitor with IC50 of 0.7 nM (hPOLθ ATPase) in ADP-glo assayss.
RP-2119 exhibits high selectivity over a panel of related ATPases, including HELQ, FANCM, BLM, and WRN (IC50s>10 uM).
RP-2119 shows strong antiproliferative activity in a panel of BRCA2-deficient cancer cell lines with IC50 of 45 and 51 nM for DLD-1 BRCA2–/– (WT) and HCT 116 BRCA2–/– (WT) respectively.
RP-2119 exhibits MMEJ activity IC50 of 54 nM in cellular MMEJ reporter assay.
RP-2119 potently inhibiting the ATPase function of the helicase-like domain of Polθ across both human and preclinical species with IC50 of <2.5/<3/<3/<1.5/<5 nM for mouse/ rat / dog / pig / chimpanzee POLθ ATPase domain in ADP-glo assays.
RP-2119 displays synergistic cytotoxicity in HCT 116 BRCA2–/– cells, leading to a pronounced loss of cell viability, when combined with PARP inhibitor olaparib, in HR-deficient cell line- and patient-derived mouse xenografts.

物理化学性质&存储条件

分子量 507.52
分子式 C24H19F2N7O2S
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-(5-(Cyclopropylethynyl)-1,3,4-thiadiazol-2-yl)-2′-(difluoromethyl)-5′-methoxy-6-(1-methyl-1H-pyrazol-3-yl)-[4,4′-bipyridine]-3-carboxamide

参考文献

1. Mochirian P, et al. J Med Chem. 2025 Sep 8. doi: 10.1021/acs.jmedchem.5c02103.

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