ART812 Datasheet | DC60279

ART812 — Datasheet

CAT. NO. DC60279

Parameter	Value
Chemical Name	ART812
CAS No.	2607138-82-7
Synonyms	2-Pyrrolidinecarboxamide, N-(3-chloro-4-fluorophenyl)-3,4-dihydroxy-N-methyl-1-[6-methyl-4-(trifluoromethyl)-2-pyridinyl]-5-oxo-, (2S,3S,4S)-;(2S,3S,4S)-N-(3-chloro-4-fluorophenyl)-3,4-dihydroxy-N-methyl-1-(6-methyl-4-(trifluoromethyl)pyridin-2-yl)-5-oxopyrrolidine-2-carboxamide;ART812
Formula	C19H16ClF4N3O4
M.Wt	461.79
SMILES	N1(C2=NC(C)=CC(C(F)(F)F)=C2)C(=O)[C@@H](O)[C@@H](O)[C@H]1C(N(C1=CC=C(F)C(Cl)=C1)C)=O
Purity	>98%
Storage	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

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].

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].

Target

Polθ:7.6 nM (IC50)

References & source

[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.

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.