DHAQ DIACETATE

Modify Date: 2024-01-12 10:15:55

DHAQ DIACETATE Structure
DHAQ DIACETATE structure
Common Name DHAQ DIACETATE
CAS Number 70711-41-0 Molecular Weight 504.53300
Density 1.45g/cm3 Boiling Point 805.7ºC at 760 mmHg
Molecular Formula C24H32N4O8 Melting Point 203-5ºC
MSDS N/A Flash Point 441.1ºC

 Use of DHAQ DIACETATE


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].

 Names

Name 9,10-Anthracenedione, 1,4-dihydroxy-5,8-bis[[2- [(2-hydroxyethyl)amino]ethyl]amino]-, diacetate (salt)

 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