ART812 is an orally active DNA polymerase Polθ inhibitor with an IC 50 value of 7.6 nM. ART812 has an IC 50 value of 240 nM for cell based microhomology-mediated end joining (MMEJ).

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

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?mm 3 )[1].

2607138-82-7

C19H16ClF4N3O4

461.8

ART812;ART812

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years