A PARP1 inhibitor (Ki = 6.3 nM); inhibits PARP1 activity in permeabilized and intact SW620 cells (IC50s = 29 and 14 nM

AG-14361 – 1 mg

Brand:
Cayman
CAS:
328543-09-5
Storage:
-20
UN-No:
Non-Hazardous - /

AG-14361 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1; Ki = 6.3 nM for the human enzyme).{43030} It inhibits PARP1 activity in permeabilized and intact SW620 cells (IC50s = 29 and 14 nM, respectively).{43031} AG-14361 (0.4 µM) potentiates the growth inhibitory effects of temozolomide (Item No. 14163) in HCT116, A2480, and CP70 cells and of the topoisomerase I inhibitor topotecan (Item No. 14129) by greater than three-fold in PARP1+/+ primary embryonic fibroblasts.{43032,43033} It slows the rejoining of camptothecin-induced DNA strand breaks.{43033} AG-14361 also inhibits cell growth in a PARP1-independent manner with GI50 values of 66 and 65 µM, respectively, in cell lines derived from PARP1+/+ and PARP1-/- mice.{43031} AG-14361 (15 mg/kg), in combination with temozolomide, leads to tumor regression in an SW620 mouse xenograft model.  

 

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SKU: 24677 - 1 mg Category:

Description

A PARP1 inhibitor (Ki = 6.3 nM); inhibits PARP1 activity in permeabilized and intact SW620 cells (IC50s = 29 and 14 nM, respectively); potentiates the growth inhibitory effects of temozolomide and topotecan in vitro at 0.4 µM; also inhibits cell growth in a PARP1-independent manner (GI50s = 66 and 65 µM for cells derived from PARP1+/+ and PARP1-/- mice, respectively); leads to tumor regression in an SW620 mouse xenograft model when used in combination with temozolomide

Formal name: 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro-imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one

Synonyms: 

Molecular weight: 320.4

CAS: 328543-09-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|DNA Repair Enzymes||Research Area|Cancer|DNA Damage and Repair|PARP

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