2923356-52-7
Chemical Structure
ART6043
Synonym(s): Polθ-IN-7
- CAS No.: 2923356-52-7
- Formula:C28H35F3N6O2
- Molecular Weight:544.61
InChIKey: JCATVBJYPBKEFM-IBVKSMDESA-N
SMILES: O=C1[C@@]2([H])N(C3=CC(C(F)(F)F)=CC(C)=N3)C(C[C@]2([H])CN(C4=C(C)C=CC=C4N1C)CCN5CCN(CC5)C)=O
Biological Activity: ART6043 (Polθ-IN-7) is an orally active, selective allosteric DNA polymerase θ (Polθ) inhibitor with an IC50 of 1.3 nM. ART6043 blocks microhomology-mediated end joining (MMEJ) by inhibiting the polymerase function of Polθ. ART6043 suppresses the survival of homologous recombination-deficient (HRD) cells and enhances the antitumor effects of PARP inhibitors. ART6043 can be used in studies of HRD tumors, including BRCA1-mutant triple-negative breast cancer, BRCA2-deficient colorectal cancer, RAD51C-deficient gastric cancer, and others[1].
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ART6043 | ART6043 (Polθ-IN-7) is an orally active, selective allosteric DNA polymerase θ (Polθ) inhibitor with an IC50 of 1.3 nM. ART6043 blocks microhomology-mediated end joining (MMEJ) by inhibiting the polymerase function of Polθ. ART6043 suppresses the survival of homologous recombination-deficient (HRD) cells and enhances the antitumor effects of PARP inhibitors. ART6043 can be used in studies of HRD tumors, including BRCA1-mutant triple-negative breast cancer, BRCA2-deficient colorectal cancer, RAD51C-deficient gastric cancer, and others. | |||||||||||||||||||||
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- [1]. Robinson HMR, et al. The pharmacological profile of ART6043, a first-in-class clinical DNA polymerase theta polymerase domain inhibitor potentiating PARP inhibitor efficacy. Clinical cancer research : an official journal of the American Association for Cancer Research. 2026 Jul 13. [Content Brief]
Keywords
