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经验公式(希尔记法):
C9H8N2O2
化学文摘社编号:
分子量:
176.17
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
SMILES string
[nH]1[c](c2c(nc1C)c(ccc2)O)=O
InChI
1S/C9H8N2O2/c1-5-10-8-6(9(13)11-5)3-2-4-7(8)12/h2-4,12H,1H3,(H,10,11,13)
InChI key
YJDAOHJWLUNFLX-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 25 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
General description
A potent inhibitor poly(ADP-ribose) polymerase (PARP; IC50 = 0.40 µM). Has been shown to potentiate the cytotoxicity of the DNA-methylating agent MTIC [5-(3-N-methyltriazen-1-yl)-imidazole-4-carboxamide] and ionizing irradiation in murine L210 leukemia cells.
A potent poly(ADP-ribose) polymerase (PARP) inhibitor (IC50 = 400 nM) that potentiates the cytotoxicity of various DNA-active agents, including the DNA-methylating compound MTIC [5-(3-N-methyltriazen-1-yl)-imidazole-4-carboxamide], the DNA strand break-inducing drug temozolomide, topotecan, bleomycin, and ionizing radiation in murine L1210 leukemia cells, Chinese hamster ovary cells, and in a variety of human tumor cell lines.
Biochem/physiol Actions
Cell permeable: no
Primary Target
PARP
PARP
Product does not compete with ATP.
Reversible: no
Target IC50: 0.4 µM against poly(ADP-ribose) polymerase (PARP)
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
This solution can be further diluted 1:100 in tissue culture medium before use.
Other Notes
Delaney, C.A., et al. 2000. Clin. Cancer Res.6, 2860.
Boulton, S., et al. 1999. Carcinogenesis20, 199.
Bowman, K.J., et al. 1998. Br. J. Cancer 78, 1269.
Griffin, R.J., et al. 1998. J. Med. Chem. 41, 5247.
Griffin, R.J., et al. 1996. Pharm. Sci. 2, 43.
Boulton, S., et al. 1995. Br. J. Cancer 72, 849.
Griffin, R.J., et al. 1995. Anticancer Drug Res. 10, 507.
Boulton, S., et al. 1999. Carcinogenesis20, 199.
Bowman, K.J., et al. 1998. Br. J. Cancer 78, 1269.
Griffin, R.J., et al. 1998. J. Med. Chem. 41, 5247.
Griffin, R.J., et al. 1996. Pharm. Sci. 2, 43.
Boulton, S., et al. 1995. Br. J. Cancer 72, 849.
Griffin, R.J., et al. 1995. Anticancer Drug Res. 10, 507.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
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