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ART812

  Cat. No.:  DC60279   Featured
Chemical Structure
2607138-82-7
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Field of application
ART-812 is a potent inhibitor of DNA polymerase Polθ (also known as Pol theta or POLQ), with an IC50 value of 7.6 nM. This indicates that ART-812 effectively inhibits the enzymatic activity of Polθ at low nanomolar concentrations. Polθ is a key enzyme involved in the microhomology-mediated end joining (MMEJ) pathway, which is an error-prone DNA repair mechanism.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2607138-82-7
Chemical Name: ART812
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
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
Formula: C19H16ClF4N3O4
M.Wt: 461.79
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
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].
Target: Polθ:7.6 nM (IC50)
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].
In Vitro: ART812 (0-40 μM) elicits Polθ inhibitor sensitivity in MDA-MB-436 SHLD2 knockout cells[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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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