Merbarone
Modify Date: 2024-01-02 23:26:20
Merbarone structure
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Common Name | Merbarone | ||
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| CAS Number | 97534-21-9 | Molecular Weight | 263.27200 | |
| Density | 1.51g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C11H9N3O3S | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
Use of MerbaroneMerbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage. Merbarone is an anticancer agent[1][2]. |
| Name | 6-hydroxy-4-oxo-N-phenyl-2-sulfanylidene-1H-pyrimidine-5-carboxamide |
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| Synonym | More Synonyms |
| Description | Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage. Merbarone is an anticancer agent[1][2]. |
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| Related Catalog | |
| Target |
topoisomerase II[1] |
| In Vitro | Merbarone (1-100 μM) inhibits L1210 cells proliferation in a concentration-dependent manner, with an IC50 of 10 μM[3]. Merbarone (10-200 μM; 10 min) inhibits DNA relaxation catalyzed by human topoisomerase IIα, with an IC50 of ∼40 μM[1]. Merbarone (25-200 μM; 6 min) blocks tyopoisomerase II-mediated DNA cleavage, with an IC50 of ∼50 μM[1]. Merbarone (100 μM; 6 min) inhibits topoisomerase II-mediated DNA cleavage in a global manner[1]. Merbarone (100 μM; 6 min) does not impair topoisomerase II•DNA binding[1]. Merbarone (200 μM; 4-16 min) does not inhibit topoisomerase II-catalyzed ATP hydrolysis[1]. |
| In Vivo | Merbarone (50 mg/kg; daily i.p. for 5 d) achieves a maximum increased life span (ILS) of 101% in P388 murine leukemia[2]. Merbarone (124 mg/kg; daily p.o. for 9 d) has anti-tumor activity in mice[2]. |
| References |
| Density | 1.51g/cm3 |
|---|---|
| Molecular Formula | C11H9N3O3S |
| Molecular Weight | 263.27200 |
| Exact Mass | 263.03600 |
| PSA | 119.39000 |
| LogP | 0.50280 |
| Index of Refraction | 1.688 |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
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| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| RIDADR | NONH for all modes of transport |
| RTECS | UV7714625 |
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Dominant lethal mutations of topoisomerase II inhibitors etoposide and merbarone in male mice: a mechanistic study.
Arch. Toxicol. 86(5) , 725-31, (2012) Two topoisomerase II inhibitors, etoposide and merbarone, were tested for the induction of dominant lethal mutations in male mice. Etoposide was administered at a dosage of 30 or 60 mg/kg. Merbarone w... |
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Merbarone: an antitumor agent entering clinical trials.
Invest. New Drugs 5(2) , 137-43, (1987) Merbarone was developed to clinical trial stage on the basis of its 'curative' activity against P388 and L1210 leukemias and moderate activity against B16 melanoma and M5076 sarcoma. Its activity appe... |
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Differential cell cycle-specificity for chromosomal damage induced by merbarone and etoposide in V79 cells.
Mutat. Res. 616(1-2) , 70-82, (2007) Merbarone, a topoisomerase II (topo II) inhibitor which, in contrast to etoposide, does not stabilize topo II-DNA cleavable complexes, was previously shown to be a potent clastogen in vitro and in viv... |
| CC-PMLSC-PW-kmcmerbarone |
| HMS2198P18 |