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PDD 00017273

Chemical Structure : PDD 00017273

CAS No.: 1945950-21-9

PDD 00017273 (PDDX-001, PDD00017273)

Catalog No.: PC-62412Not For Human Use, Lab Use Only.

PDD 00017273 (PDDX-001) is the first-in-class, selective inhibitor of poly(ADP-ribose) glycohydrolase (PARG) with Kd, biochemical EC50 of 1.45 nM, 26 nM.

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Biological Activity

PDD 00017273 (PDDX-001) is the first-in-class, selective inhibitor of poly(ADP-ribose) glycohydrolase (PARG) with Kd, biochemical EC50 of 1.45 nM, 26 nM.
PDD 00017273 inhibits the proliferation of ZR-75-1 cells and MDA-MB-436 with IC50 of 0.2 and 0.8 uM.
PDD 00017273 inhibits DNA repair with differential pharmacology to olaparib; shows no activity against CYP450 isoforms.
PDD 00017273 possesses good aqueous solubility and suitable for in vivo studies.

Physicochemical Properties

M.Wt 514.619
Formula C23H26N6O4S2
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

1-[(1,3-Dimethyl-1H-pyrazol-5-yl)methyl]-1,2,3,4-tetrahydro-N-(1-methylcyclopropyl)-3-[(2-methyl-5-thiazolyl)methyl]-2,4-dioxo-6-quinazolinesulfonamide

References

1. James DI, et al. ACS Chem Biol. 2016 Nov 18;11(11):3179-3190.

2. Gravells P, et al. DNA Repair (Amst). 2017 Apr;52:81-91.

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