Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro-
- Product Name
- Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro-
- CAS No.
- 328543-09-5
- Chemical Name
- Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro-
- Synonyms
- CS-421;AG14361;AG14361;AG 14361;AG14361; AG-14361; AG 14361.;AG-14361 AG14361 PARP-1 inhibitor;inhibit,PARP,Inhibitor,poly ADP ribose polymerase,AG14361;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-
- CBNumber
- CB72525863
- Molecular Formula
- C19H20N4O
- Formula Weight
- 320.39
- MOL File
- 328543-09-5.mol
Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro- Property
- Density
- 1.27
- storage temp.
- Store at -20°C
- solubility
- insoluble in H2O; ≥10.14 mg/mL in EtOH with gentle warming and ultrasonic; ≥16 mg/mL in DMSO
- form
- solid
- pka
- 14.05±0.20(Predicted)
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- 24677
- Product name
- AG-14361
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 24677
- Product name
- AG-14361
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $193
- Updated
- 2024/03/01
- Product number
- 24677
- Product name
- AG-14361
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $341
- Updated
- 2024/03/01
- Product number
- 24677
- Product name
- AG-14361
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $745
- Updated
- 2024/03/01
- Product number
- KIN0000939
- Product name
- AG-14361
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $597
- Updated
- 2021/12/16
Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro- Chemical Properties,Usage,Production
Definition
ChEBI: LSM-1988 is a member of benzimidazoles.
Biological Activity
ag-14361 is a selective inhibitor of parp-1 with ki50 valueparp1 is a member of prap family and plays an important role in many cellular processes, such as dna repair, programmed cell death. it has been revealed that parp1 is abnormally expressed in a variety of cancers and many parp inhibitors have been developed as the anti-tumor drugs [1] [2] [3, 4].ag-14361 is a potent parp-1 inhibitor. when exposed hr and brca2-defective cells and parental cells to ag-14361, hr-defective cells were hypersensitive to the ag-14361 even at non-cytotoxic concentrations and lacking brca2 made the cells more sensitive to ag-14361 [5]. in human k562 cells, ag14361 treatment for 16 hours resulted in significant (~2-fold) potentiation of camptothecin-induced growth inhibition (gi50, 16 hours, camptothecin + ag14361 2.4 ± 0.1 nmol/l), cytotoxicity (lc50, camptothecin + ag14361 2.77 ± 0.55 nmol/l) and dna single-strand breaks via inhibiting parp-1 [1]. when tested with mmr-proficient (hct-ch3, a2780, and cp70-ch3) and mmr-deficient (hct116, cp70, and cp70-ch2) cells, mmr-proficient cells were more sensitivity to temozolomide compared with mmr-deficient cells after exposed to ag-14361 which inhibited parp1 activity [2].in mouse model xenografted with brca2-deficient and brca-2 proficient tumor cells, brca2 deficiency group had more response even completely regressed tumor compared with brca-2 proficient group when treated with ag-14361 [5].
target
PARP1
References
[1]. smith, l.m., 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): p. 8449-57.
[2]. curtin, n.j., 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): p. 881-9.
[3]. calabrese, c.r., et al., anticancer chemosensitization and radiosensitization by the novel poly(adp-ribose) polymerase-1 inhibitor ag14361. j natl cancer inst, 2004. 96(1): p. 56-67.
[4]. veuger, s.j., et al., radiosensitization and dna repair inhibition by the combined use of novel inhibitors of dna-dependent protein kinase and poly(adp-ribose) polymerase-1. cancer res, 2003. 63(18): p. 6008-15.
[5]. kyle, s., et al., exploiting the achilles heel of cancer: the therapeutic potential of poly(adp-ribose) polymerase inhibitors in brca2-defective cancer. br j radiol, 2008. 81 spec no 1: p. s6-11.
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Raw materials
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View Lastest Price from Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro- manufacturers
- Product
- Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro- 328543-09-5
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 98%
- Supply Ability
- 1lg; 2kg; 5kg; 10kg; 100kg
- Release date
- 2019-08-31