ART812 是一种口服有效的 DNA 聚合酶 Polθ 抑制剂，IC50 值为 7.6 nM。ART812 对基于细胞的微同源介导的末端连接 (MMEJ) 的 IC50 值为 240 nM。
货号:ajcx37590
CAS:2607138-82-7
分子式:C19H16ClF4N3O4
分子量：461.79
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.