AZ6102

Research use only, not for human use.

AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells.

AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows 5 nM Wnt pathway inhibition in DLD-1 cells. AZ6102 can be formulated well in a clinically relevant intravenous solution at 20 mg/mL, has demonstrated good pharmacokinetics in preclinical species, and shows low Caco2 efflux to avoid possible tumor resistance mechanisms. The canonical Wnt pathway plays an important role in embryonic development, adult tissue homeostasis, and cancer. Germline mutations of several Wnt pathway components, such as Axin, APC, and ?-catenin, can lead to oncogenesis. Inhibition of the poly(ADP-ribose) polymerase (PARP) catalytic domain of the tankyrases (TNKS1 and TNKS2) is known to inhibit the Wnt pathway via increased stabilization of Axin.

AZ6102 is a potent dual TNKS1 and TNKS2 inhibitor, with IC50s of 3 nM and 1 nM, respectively. AZ6102 alao has 100-fold selectivity against other PARP family enzymes, with IC50s of 2.0 μM, 0.5 μM, and >3 μM, for PARP1, PARP2, and PARP6, respectively. AZ6102 shows Wnt pathway inhibition in DLD-1 cells.

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AZ6102 | AZ-6102 | AZ 6102

Cytoskeleton/Cell Adhesion Molecules

Glucokinase

TNKS1| TNKS2

Cancer

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1645286-75-4

428.53

C25H28N6O

>98% (HPLC)

DMSO : ≥ 29 mg/mL; 67.67 mM

C[C@@H]1CN(c2ncc(c3ccc(c4nc(=O)c5ccn(C)c5[nH]4)cc3)c(C)c2)C[C@H](C)N1

2-(4-(6-((3R,5S)-3,5-dimethylpiperazin-1-yl)-4-methylpyridin-3-yl)phenyl)-7-methyl-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one

(-20℃)

With Ice Pack

≥ 2 years