compound introduction
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. Form:Solid IC50& Target:Polθ 7.6 nM (IC 50 )
