ART812

Modify Date: 2024-01-08 15:50:16

ART812 Structure
ART812 structure
Common Name ART812
CAS Number 2607138-82-7 Molecular Weight 461.79
Density N/A Boiling Point N/A
Molecular Formula C19H16ClF4N3O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of ART812


ART812 is a 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].

 Names

Name ART812

 ART812 Biological Activity

Description ART812 is a 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].
Related Catalog
Target

Polθ:7.6 nM (IC50)

In Vitro ART812 (0-40 μM) elicits Polθ inhibitor sensitivity in MDA-MB-436 SHLD2 knockout cells[1].
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 mm3)[1].
References

[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.

 Chemical & Physical Properties

Molecular Formula C19H16ClF4N3O4
Molecular Weight 461.79