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ART812

Chemical Structure : ART812

CAS No.: 2607138-82-7

ART812 (ART-812)

Catalog No.: PC-49362Not For Human Use, Lab Use Only.

ART812 (ART-812) is a selective small molecule DNA polymerase theta (Polθ) in vivo probe with IC50 of 7.6 nM, and IC50 of 240 nM for cell based microhomology-mediated end joining (MMEJ).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

ART812 (ART-812) is a selective small molecule DNA polymerase theta (Polθ) in vivo probe with IC50 of 7.6 nM, and IC50 of 240 nM for cell based microhomology-mediated end joining (MMEJ).
ART812 recapitulates the phenotype of Polθ loss and is efficacious in a model of PARP inhibitor resistant TNBC in vivo.

Physicochemical Properties

M.Wt 461.798
Formula C19H16ClF4N3O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(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

References

1. Martin L Stockley, et al. J Med Chem. 2022 Oct 6. doi: 10.1021/acs.jmedchem.2c01142.

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