2922287-81-6
Chemical Structure
RP-2119
- CAS No.: 2922287-81-6
- Formula:C24H19F2N7O2S
- Molecular Weight:507.52
InChIKey: GSOUEPGHLLFNOU-UHFFFAOYSA-N
SMILES: O=C(C1=C(C=C(N=C1)C2=NN(C=C2)C)C3=CC(C(F)F)=NC=C3OC)NC4=NN=C(S4)C#CC5CC5
Biological Activity: RP-2119 is an orally bioactive Polymerase Theta (Polθ) inhibitor, with an IC50 of 0.7 nM against human Polθ ATPase. RP-2119 reduces Polθ activity and exerts antiproliferative effects in BRCA2-deficient cancer cells. RP-2119 exhibits antitumor activity in BRCA2-deficient cancer cell xenograft mouse models. RP-2119 can be used for the research of cancer and homologous recombination-deficient cancers, including brca1/brca2-mutant cancers and shld2-mutant cancers[1][2].
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RP-2119 | 99.94% | RP-2119 is an orally bioactive Polymerase Theta (Polθ) inhibitor, with an IC50 of 0.7 nM against human Polθ ATPase. RP-2119 reduces Polθ activity and exerts antiproliferative effects in BRCA2-deficient cancer cells. RP-2119 exhibits antitumor activity in BRCA2-deficient cancer cell xenograft mouse models. RP-2119 can be used for the research of cancer and homologous recombination-deficient cancers, including brca1/brca2-mutant cancers and shld2-mutant cancers. | ||||||||||||||||||||
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- [1]. Bingcan Liu, et al. N-(5-substituted-[(I,3,4-thiadiazolyl) or(I,3-thiazolyl)](substituted)carboxamide compoundspharmaceutical compositions, and methods of preparing the amide compounds and of their use. Wo2024069592A1.2024.04.04.
- [2]. Mochirian P, et al. The Discovery of RP-2119: A Potent, Selective, and Orally Bioavailable Polθ ATPase Inhibitor. J Med Chem. 2025;68(18):19726-19745. [Content Brief]
Keywords
