Abstract |
4,4'-Dihydroxybenzophenone-2,4-dinitrophenylhydrazone (A-007) is being evaluated for its anticancer activities. Acute, subacute and chronic oral, dermal, opthalmic and dermal LD50 and acceptance studies in adult mice, rats, rabbits and monkeys demonstrated some vomiting at 5 g/kg doses in monkeys but otherwise no unacceptable toxicities. In vitro, T.I. for A-007 were calculated using murine bone marrow GM-CFC and human cancer cell lines. A relative oral bioavailability factor of 2% was calculated for rats and monkeys for plasma A-007. Non-compartmental pharmacokinetic analysis suggests enterohepatic circulation. Plasma A-007 could not be detected after applying a 0.25% gel topically. Generally, A-007 is well tolerated.
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Authors | L R Morgan, A H Rodgers, D Fan, K Soike, M Ratterree, B W Sartin, T J Harrison |
Journal | In vivo (Athens, Greece)
(In Vivo)
1997 Jan-Feb
Vol. 11
Issue 1
Pg. 29-37
ISSN: 0258-851X [Print] Greece |
PMID | 9067770
(Publication Type: Comparative Study, Journal Article, Research Support, U.S. Gov't, P.H.S.)
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Chemical References |
- 4,4'-dihydroxybenzophenone-2,4-dinitrophenylhydrazone
- Antineoplastic Agents
- Hydrazones
- Phenols
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Topics |
- Administration, Oral
- Animals
- Antineoplastic Agents
(pharmacokinetics, toxicity)
- Bone Marrow Cells
- Breast Neoplasms
- Carcinogenicity Tests
- Chlorocebus aethiops
- Colonic Neoplasms
- Dose-Response Relationship, Drug
- Eye Infections
(chemically induced)
- Female
- Fibroblasts
(cytology, drug effects)
- Humans
- Hydrazones
(pharmacokinetics, toxicity)
- Injections, Intraperitoneal
- Kidney Neoplasms
- Lung Neoplasms
- Male
- Melanoma
- Mice
- Mice, Inbred Strains
- Phenols
(pharmacokinetics, toxicity)
- Rabbits
- Rats
- Rats, Sprague-Dawley
- Reproduction
(drug effects)
- Skin Diseases
(chemically induced)
- Tumor Cells, Cultured
(drug effects)
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