ART812 |
| Catalog No.GC64426 |
ART812 est un inhibiteur de l'ADN polymérase Polθ actif par voie orale avec une valeur IC50 de 7,6 nM. ART812 a une valeur IC50 de 240 nM pour la jonction d'extrémité médiée par microhomologie cellulaire (MMEJ).
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Cas No.: 2607138-82-7
Sample solution is provided at 25 µL, 10mM.
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ART812 is an orally active 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].
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 mm3)[1].
[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.
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