ART812

Names

[ Name ]:
ART812

Biological Activity

[Description]:

ART812 is a DNA polymerase Polθ inhibitor with an IC50 value of 7.6 nM. ART812 has an IC50 value of 240 nM for cell based microhomology-mediated end joining (MMEJ)[1][2].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Others >> Others

[Target]

Polθ:7.6 nM (IC50)

[In Vitro]

ART812 (0-40 μM) elicits Polθ inhibitor sensitivity in MDA-MB-436 SHLD2 knockout cells[1].

[In Vivo]

ART812 (100 mg/kg; p.o. daily for 76 days) shows significant tumour inhibition in rats bearing established MDA-MB-436 BRCA1/SHLD2 defective tumours (volume 250-350 mm3)[1].

[References]

[1]. Zatreanu D, et al. Polθ inhibitors elicit BRCA-gene synthetic lethality and target PARP inhibitor resistance. Nat Commun. 2021 Jun 17;12(1):3636.

[2]. Peter BLENCOWE, et al. Preparation of heterocyclic compounds for use in the treatment of cancer. WO2021028643 A1.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₉H₁₆ClF₄N₃O₄

[ Molecular Weight ]:
461.79

Related Compounds

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