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
- Molecular Weight:
- 320.39
- MDL Number:
- MFCD18385009
- MOL File:
- 328543-09-5.mol
- MSDS File:
- SDS
Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro- Properties
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 |
FDA UNII | 48N0U0K50I |
Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro- price More Price(22)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Cayman Chemical | 24677 | AG-14361 ≥98% | 328543-09-5 | 1mg | $44 | 2024-03-01 | Buy |
Cayman Chemical | 24677 | AG-14361 ≥98% | 328543-09-5 | 5mg | $193 | 2024-03-01 | Buy |
Cayman Chemical | 24677 | AG-14361 ≥98% | 328543-09-5 | 10mg | $341 | 2024-03-01 | Buy |
Cayman Chemical | 24677 | AG-14361 ≥98% | 328543-09-5 | 25mg | $745 | 2024-03-01 | Buy |
American Custom Chemicals Corporation | KIN0000939 | AG-14361 95.00% | 328543-09-5 | 5MG | $597 | 2021-12-16 | Buy |
Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro- Chemical Properties,Uses,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.
Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro- Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32835 | 60 |
career henan chemical co | +86-0371-86658258 +8613203830695 | sales@coreychem.com | China | 29899 | 58 |
Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28180 | 58 |
Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 23430 | 58 |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10522 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
Hunan Jibang Biological Technology Co., LTD | +8613776644403 | sales02@kingboomtech.com | China | 1806 | 58 |
Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3136 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
View Lastest Price from Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro- manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
---|---|---|---|---|---|---|---|---|
2019-09-02 | Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro-
328543-09-5
|
US $1.00-1.00 / KG | 1KG | 98% | 1lg; 2kg; 5kg; 10kg; 100kg | Career Henan Chemical Co |
- Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro-
328543-09-5
- US $1.00-1.00 / KG
- 98%
- Career Henan Chemical Co