ART812 chemical structure
Chemical structureResearch use only
CAT. NO. DC60279Featured

ART812

Pack Sizes & Prices

TotalUS$700
We match the best price and quality on market.
Product overview

Description & Application

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].

ParameterValue
Chemical NameART812
CAS No.2607138-82-7
Synonyms2-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
FormulaC19H16ClF4N3O4
M.Wt461.79
SMILESN1(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%
Storage2 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.

Product documentation

View online datasheetRequest COA / MSDS

Refer to the certificate supplied with your lot for batch-specific release results.

Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Solution calculator

Related research products

Fluzoparib chemical structureDC22228

Fluzoparib

Fluzoparib (SHR-3162) is a novel, potent and orally available inhibitor of PARP; potently inhibited PARP1 enzyme activity and induced DNA double-strand breaks, G2/M arrest and apoptosis in homologous recombination…

View activity & prices
PF-670462 chemical structureDC2086

PF-670462

PF-670462 is a potent and selective inhibitor of casein kinase (CK1ε and CK1δ), with IC50s of 7.7 nM and 14 nM, respectively.

View activity & prices
PBIT chemical structureDC7550

PBIT

PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1(JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1 ) histone demethylase an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with…

View activity & prices
Fenoldopam (mesylate) chemical structureDC9424

Fenoldopam (mesylate)

Fenoldopam(SKF 82526) mesylate is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist.Target: D1 ReceptorFenoldopam is a selective dopamine-1 (DA1) agonist with…

View activity & prices
PKG drug G1 chemical structureDC10821

PKG drug G1

PKG drug G1 targets C42 of PKG Iα. PKG drug G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.

View activity & prices

Cart

Request quotation