2-[4-[(Dimethylamino)methyl]phenyl]-5,6-dihydroimidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one

Name	AG14361
Synonyms	AG14361 AG 14361 2-(4-((dimethylamino)methyl)phenyl)-5,6 dihydropyrazino[3,2,1-ij]quinazolin-7(3H)-one 1-(4-((Dimethylamino)methyl)phenyl)-8,9-dihydro-2,7,9a-triazabenzo[cd]azulen-6(7H)-one 2-[4-[(Dimethylamino)methyl]phenyl]-5,6-dihydroimidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro- 2-(4-((dimethylamino)methyl)phenyl)-5,6 dihydropyrazino[3,2,1-ij]quinazolin-7(3H)-one (AG14361) AG 14361 2-[4-[(Dimethylamino)methyl]phenyl]-5,6-dihydroimidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one
CAS	328543-09-5

Molecular Formula	C19H20N4O
Molar Mass	320.39
Density	1.27
pKa	14.05±0.20(Predicted)
Storage Condition	-20℃
In vitro study	AG14361 is at least 1 × 10 more potent than Benzamides. AG14361 enhances the growth inhibitory and toxic effects of topoisomerase I poison. AG14361 improves the persistence of Camptothecin-induced DNA single-strand breaks.
In vivo study	AG14361 treatment of mice bearing LoVo xenografts followed by statistical irradiation significantly increased sensitivity to radiation therapy. AG14361 acts on the transplanted tumor and statistically significantly increases blood flow, therefore, it may promote drug delivery to the transplanted tumor. In Vivo, AG14361 treated with non-toxic doses increased the growth delay of LoVo xenografts induced by Irinotecan, X-ray irradiation, and Temozolomide by 2 to 3 times. Pharmacodynamic experiments showed that AG14361 was injected intraperitoneally at a dose of 10 mg/kg to treat SW620 transplanted tumor for at least 4 hours, and more than 75% of the PARP-1 activity was inhibited.

Last Update：2024-01-02 23:10:35

in cell-free assay

biological activity	AG-14361 is a potent PARP1 inhibitor with a Ki below 5 nM, at least 1000 times more potent than benzamide. AG14361 is a potent PARP1 inhibitor, Ki
characteristics	AG14361 is the first potent PARP-1 inhibitor with selectivity and in vivo activity, enhanced chemotherapy and radiation therapy for human cancer.
Target	Value
PARP1 (Cell-free assay)	<5 nM(Ki)

Last Update：2024-04-09 20:52:54

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CAS: 328543-09-5
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Product Name: AG14361 Visit Supplier Webpage Request for quotation
CAS: 328543-09-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

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2-[4-[(Dimethylamino)methyl]phenyl]-5,6-dihydroimidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one Request for Quotation