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ART558

Chemical Structure : ART558

CAS No.: 2603528-97-6

ART558 (ART-558)

货号: PC-72020Not For Human Use, Lab Use Only.

ART558 (ART-558) is a highly potent, selective, allosteric inhibitor of the polymerase function of DNA polymerase Polθ with IC50 of 7.9 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ART558 (ART-558) is a highly potent, selective, allosteric inhibitor of the polymerase function of DNA polymerase Polθ with IC50 of 7.9 nM.
ART558 does not inhibit other human DNA polymerases, namely Polα, Polγ, Polη and Polν, as well as a panel of 78 oncology-focussed kinases, including PARP1 and PARP2.
ART558 inhibits the major Polθ-mediated DNA repair process, Theta-Mediated End Joining, without targeting Non-Homologous End Joining (NHEJ).
ART558 elicits DNA damage and synthetic lethality in BRCA1- or BRCA2-mutant tumour cells and enhances the effects of PARP inhibitor Olaparib.

物理化学性质&存储条件

分子量 418.42
分子式 C21H21F3N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO (4.2 mg/mL)

Chemical Name/SMILES

(2S)-1-(3-cyano-6-methyl-4-(trifluoromethyl)pyridin-2-yl)-3-hydroxy-N-methyl-N-(m-tolyl)pyrrolidine-2-carboxamide

参考文献

1. Diana Zatreanu, et al. Nat Commun. 2021 Jun 17;12(1):3636.

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