3035072-49-9
Chemical Structure
RTx-161
- CAS No.: 3035072-49-9
- Formula:C21H18F7N3O4
- Molecular Weight:509.37
InChIKey: SMVCNKJTRUVRLZ-UHFFFAOYSA-N
SMILES: FC(F)(F)C1=CC(N2CCN(CCO)C2=O)=C(OC(N(C3=CC=C(F)C=C3)C)=O)C(C(F)(F)F)=C1
Biological Activity: RTx-161 is a DNA polymerase θ inhibitor with an IC50 of 4.1 nM. RTx-161 induces DNA damage, PARP cleavage, apoptosis, and selectively kills homologous recombination-deficient (HRD) cells. RTx-161 acts synergistically with PARP inhibitors to suppress PARP inhibitor resistance in cancer cells. RTx-161 can be used for the research of BRCAG12C mutant cancer and HR-deficient cancers[1][2].
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RTx-161 | 98.0% | RTx-161 is a DNA polymerase θ inhibitor with an IC50 of 4.1 nM. RTx-161 induces DNA damage, PARP cleavage, apoptosis, and selectively kills homologous recombination-deficient (HRD) cells. RTx-161 acts synergistically with PARP inhibitors to suppress PARP inhibitor resistance in cancer cells. RTx-161 can be used for the research of BRCAG12C mutant cancer and HR-deficient cancers. | ||||||||||||||||||||
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- [1]. Chandramouly G, et al. RTx-303, an Orally Bioavailable Polθ Polymerase Inhibitor That Potentiates PARP Inhibitors in BRCA Mutant Tumors. J Med Chem. 2025;68(21):22196-22215. [Content Brief]
- [2]. Fried W, et al. Discovery of a small-molecule inhibitor that traps Polθ on DNA and synergizes with PARP inhibitors. Nat Commun. 2024;15(1):2862. Published 2024 Apr 5. [Content Brief]
Keywords
