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)
In Vitro
ART812 (0-40 μM) elicits Polθ inhibitor sensitivity in MDA-MB-436 SHLD2 knockout cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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?mm 3 ) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
