For research use only. Not for therapeutic Use.
ART812 is an orally active 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].
ART812 (0-40 μM) elicits Polθ inhibitor sensitivity in MDA-MB-436 SHLD2 knockout cells[1].
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].
| Catalog Number | I044429 |
| CAS Number | 2607138-82-7 |
| Synonyms | (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 |
| Molecular Formula | C19H16ClF4N3O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C19H16ClF4N3O4/c1-8-5-9(19(22,23)24)6-13(25-8)27-14(15(28)16(29)18(27)31)17(30)26(2)10-3-4-12(21)11(20)7-10/h3-7,14-16,28-29H,1-2H3/t14-,15-,16-/m0/s1 |
| InChIKey | YJJOABOMFPGRED-JYJNAYRXSA-N |
| SMILES | CC1=CC(=CC(=N1)N2C(C(C(C2=O)O)O)C(=O)N(C)C3=CC(=C(C=C3)F)Cl)C(F)(F)F |
| Reference | [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. |
