| 产品名称 | AG-14361 - Inhibitors / Activators - PARP(s) |
| 产品货号 | 27602-3 |
| 产品价格 | 现货询价，电话：010-67529703 |
| 产品规格 | 50 mg |
| 产品品牌 | bpsbioscience |
| 产品概述 | |
| 产品详情 |
MW: 320.4 Da
CAS Registry #: 328543-09-5
Formula: C19H20N4O
Target: PARP1
Background: A 17-hour exposure of A549 cells to 0.4 µM AG14361 does not change the expression of the 6800 genes. Thus, although 0.4 µM AG14361 inhibits cellular PARP-1 activity by more than 85%, it essentially does not change gene expression and cell proliferation, indicating that the cellular effects of this low concentration of AG14361 are specific for PARP-1 inhibition. Higher, growth-inhibitory concentrations of AG14361 affects gene expression, but these effects are not likely to be related to PARP-1 inhibition because cell proliferation is affected equally in PARP-/- and PARP-1+/+ cells.
Description: AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM. It is at least 1000-fold more potent than the benzamides. AG14361 treatment before irradiation statistically significantly increases the sensitivity to radiation therapy. AG14361 enhances the growth-inhibitory and cytotoxic effects of topoisomerase I poisons and increases the persistence of camptothecin-induced DNA single-strand breaks.
Synonym(s): 1-(4-((dimethylamino)methyl)phenyl)-8,9-dihydro-2,7,9a-triazabenzo[cd]azulen-6(7H)-one
Purity: ≥98% by HPLC Biological Activity: The IC50 for AG14361 is 29 nM in permeabilized SW620 cells and 14 nM in intact SW620 cells.
Solubility: Soluble in DMSO. Solubility in water or ethanol is <1 mg/ml
Storage / Stability: Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day. Reference(s): 1. Smith LM, et al. Clin Cancer Res. 2005 Dec 1;11(23):8449-57.
2. Curtin NJ, et al. Clin Cancer Res. 2004 Feb 1;10(3):881-9. 3. Calabrese CR, et al. J Natl Cancer Inst. 2004 Jan 7;96(1):56-67. Scientific Category: PARP Inhibitor
Product Type: Inhibitor
Data shown is lot-specific. Contact us for specific information on other lots.
|
| 产品资料 |
