AG14361 was a potent PARP1 inhibitor with Ki <5 nM in the cell-free assay. It is at least 1000 times more effective than benzamides.

 

Brand: BCM

 

Target: PARP

 

Signaling Pathways: Chromatin/Epigenetic; DNA Damage/DNA Repair

 

In Vitro: "At non-toxic doses,AG14361 increased irinotecan, X-ray irradiation, and temozolomide induced tumor growth delay in LoVo xenografts by two to three times." In SW620 xenograft tumors, treatment with AG14361 (10 mg/kg,i.p.) for more than 4 hours inhibited PARP-1 activity by more than 75%. In mice bearing LoVo xenograft tumors, treatment with AG14361 before statistical irradiation significantly increased the sensitivity to radiotherapy. In transplanted tumors,AG14361 significantly increased blood flow, and thus may facilitate drug delivery to transplanted tumors.

 

pKa: 14.05±0.20(Predicted)

 

Solubility: Soluble in DMSO; Soluble in Ethanol. Insoluble in Water.

 

Isomeric SMILES: CN(C)CC1=CC=C(C=C1)C2=NC3=CC=CC4=C3N2CCNC4=O  

 

InChIKey: SEKJSSBJKFLZIT-UHFFFAOYSA-N  

 

InChI: InChI=1S/C19H20N4O/c1-22(2)12-13-6-8-14(9-7-13)18-21-16-5-3-4-15-17(16)23(18)11-10-20-19(15)24/h3-9H,10-12H2,1-2H3,(H,20,24)

 

Attribute
[Chem Name]	2-[4-[(dimethylamino)methyl]phenyl]-1,3,10-triazatricyclo[6.4.1.04,13]trideca-2,4,6,8(13)-tetraen-9-one
[CAS No.]	328543-09-5
[MDL No.]	MFCD18385009
[Formula]	C19H20N4O
[Molecular]	320.39
[Form]	Solid Powder
[Storage]	Sealed in dry. Store in freezer, under -20°C
[Synonym]	AG-14361; AG14361; AG 14361

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