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
Product does not compete with ATP.
Reversible: no
Target IC50: 0.4 µM against poly(ADP-ribose) polymerase (PARP)
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Preparation Note
This solution can be further diluted 1:100 in tissue culture medium before use.
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 12352200
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 493800-5MG
- CAS:
- 90417-38-2
