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Cat. No. Name Size Price Add Cart
KI3345AG143615 mg$300

Chemical Characteristic

Product NameAG14361
CAS No.328543-09-5
Molecular Weight 320
FormulaC19H20N4O
Chemical Name1-(4-((dimethylamino)methyl)phenyl)-8,9-dihydro-2,7,9a-triazabenzo[cd]azulen-6(7H)-one
Smilesn12CCNC(=O)c3c1c(ccc3)nc2c1ccc(cc1)CN(C)C
Chemical Structure

Biological activities

AG14361 is a potent PARP1 inhibitor with Ki of <5 nM. AG14361 is at least 1000-fold more potent than the benzamides. AG14361 inhibits the PARP-1 activity in permeabilized SW620 cells and intact SW620 cells with IC50s of 29 and 14 nM, respectively. AG14361 inhibits the growth of cultured A549, LoVo, and SW620 cells with GI50s of 14, 11.2, and more than 20 µ M, respectively. AG14361 (0.4 µ M) increases the antiproliferative activity of temozolomide by 5.5-fold and topotecan by 1.6-fold in LoVo cells. AG14361 also inhibits recovery from potentially lethal γ-radiation damage in LoVo cells by 73% in vitro.[1] In vitro, AG14361 enhances temozolomide activity in mismatch repair (MMR)-proficient (HCT-Ch3, A2780, and CP70-ch3) and MMR-deficient (HCT116, CP70, and CP70-ch2) cells by 1.5-fold to 3.3-fold and 3.7-fold tp 5.2-fold potentiation, respectively.[2] In mouse embryonic fibroblasts, AG14361 treatment leads to a >3-fold sensitization of PARP-1+/+ cells to topotecan compared with a <1.4-fold sensitization in PARP-1-/- cells. In human leukemia K562 cells, AG14361 increases a 2-fold sensitization to camptothecin-induced cytotoxicity.[3] AG14361 also greatly potentiates camptothecin-mediated cytotoxicity in a panel of DNA repair-deficient Chinese hamster ovary cells, except the base excision repair-deficient EM9 cells.[3] In vivo in CD-1 nude mice, nontoxic doses of AG14361 (at 5 or 15 mg/kg) increases the delay of LoVo xenograft growth induced by irinotecan, x-irradiation, or temozolomide by 2- to 3 fold. Moreover, AG14361 treatment in combination with temozolomide leads to complete regression of SW620 xenograft tumors in vivo.[1]

Protocols

In vitro: Prior to use, AG14361 is dissolved in DMSO.[2]

References

[1] Calabrese CR, et al. Anticancer chemosensitization and radiosensitization by the novel poly(ADP-ribose) polymerase-1 inhibitor AG14361. J Natl Cancer Inst. 2004, 96(1): 56-67.
[2] Curtin NJ, et al. Novel poly(ADP-ribose) polymerase-1 inhibitor, AG14361, restores sensitivity to temozolomide in mismatch repair-deficient cells. Clin Cancer Res. 2004, 10(3): 881-889.
[3] Smith LM, et al. The novel poly(ADP-Ribose) polymerase inhibitor, AG14361, sensitizes cells to topoisomerase I poisons by increasing the persistence of DNA strand breaks. Clin Cancer Res. 2005, 11(23): 8449-8457.

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