ART812 Datasheet DC Chemicals
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Cat.No DC60279
Name ART812

Chemical Properties

CAS 2607138-82-7
Formula C19H16CLF4N3O4
MW 461.79
Storage 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological activity

Description CAS NO.：2607138-82-7
Product 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
EINEC:
Molecular Formula：C19H16CLF4N3O4
Molecular Weight：461.79
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].
Kinase Assay
Cell Assay
Animal Administration

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.
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