DHAQ DIACETATE
Names
[ CAS No. ]:
70711-41-0
[ Name ]:
DHAQ DIACETATE
Biological Activity
[Description]:
Mitoxantrone diacetate is a potent topoisomerase II inhibitor. Mitoxantrone diacetate also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone diacetate induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone diacetate shows antitumor activity[1][2][3][4]. Mitoxantrone diacetate also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively[5].
[Related Catalog]:
[Target]
IC50: 8.5 μM (PKC)[1]
[In Vitro]
Mitoxantrone diacetate inhibits PKC in a competitive manner with respect to histone H1, and its Ki value is 6.3 μM and in a non-competitive manner with respect to phosphatidylserine and ATP[1]. Mitoxantrone diacetate (0.5 μg/mL, 48 h) induces a decrease in B-CLL cells. Mitoxantrone diacetate induces DNA fragmentation and the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), demonstrating that the cytotoxic effect of Mitoxantrone diacetate is due to induction of apoptosis[2]. Mitoxantrone diacetate shows cytotoxicity to human breast carcinoma cell lines MDA-MB-231 and MCF-7 with IC50 values of 18 and 196 nM, respectively[3].
[In Vivo]
Mitoxantrone diacetate (IP, 0-3.2 mg/kg/day) produces a statistically significant number of 60-day survivors at 1.6 mg/kg in mice with IP implanted L1210 leukemia[4]. Mitoxantrone diacetate (IV, 0-3.2 mg/kg/day) shows effective antitumor activities and produces a 60% ILS (increase in lifespan) at 3.2 mg/kg in SC implanted Lewis lung carcinoma[4].
Chemical & Physical Properties
[ Density]:
1.45g/cm3
[ Boiling Point ]:
805.7ºC at 760 mmHg
[ Melting Point ]:
203-5ºC
[ Molecular Formula ]:
C24H32N4O8
[ Molecular Weight ]:
504.53300
[ Flash Point ]:
441.1ºC
[ Exact Mass ]:
504.22200
[ PSA ]:
200.48000
[ LogP ]:
0.87950
Toxicological Information
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- CB5749000
- CHEMICAL NAME :
- Anthraquinone, 5,8-bis((2-((2-hydroxyethyl)amino)ethyl)amino)-1,4-di hydroxy-, 1,4-diacetate (salt)
- CAS REGISTRY NUMBER :
- 70711-41-0
- LAST UPDATED :
- 199410
- DATA ITEMS CITED :
- 6
- MOLECULAR FORMULA :
- C22-H28-N4-O6.2C2-H4-O2
- MOLECULAR WEIGHT :
- 564.66
- WISWESSER LINE NOTATION :
- L C666 BV IVJ DOV1 GOV1 KM2M2Q NM2M2Q
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 61300 ug/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 25 mg/kg
- TOXIC EFFECTS :
- Vascular - BP lowering not characterized in autonomic section Cardiac - EKG changes not diagnostic of specified effects Cardiac - cardiac output
MUTATION DATA
- TYPE OF TEST :
- Sister chromatid exchange
- TEST SYSTEM :
- Rodent - hamster Ovary
- DOSE/DURATION :
- 10 nmol/L
- REFERENCE :
- CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 41,376,1981