Drug

D0008 | Arsenic trioxide

Molecular Formula As2O3
Molecular Weight 197.841
Structure
State solid
Route of elimination Trivalent arsenic is mostly methylated in humans and excreted in urine.
Protein binding 75% bound
Trade names Trisenox
Description chemotherapeutic agent of idiopathic function

L

L01XX27 Arsenic trioxide


[L01XX] Other antineoplastic agents


[L01X] OTHER ANTINEOPLASTIC AGENTS


[L01] ANTINEOPLASTIC AGENTS


[L] Antineoplastic and immunomodulating agents


L01XC06 Cetuximab


[L01XC] Monoclonal antibodies


[L01X] OTHER ANTINEOPLASTIC AGENTS


[L01] ANTINEOPLASTIC AGENTS


[L] Antineoplastic and immunomodulating agents


Toxicity Dose Time Species Model Method Action Positive criterion Reference
MEMBRANE POTENTIAL 237.9 µM 30 mins mouse liver mitochondria Rh123 fluorescence (excitation 485 nm, emission 535 nm) are recorded using a fluorescence multi-well plate reader (mCICCP (20 µM) treatments was considered as the 100% baseline for ΔΨm loss) decrease EC20 36
RESPIRATION < 50 µM 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Rotenone (2µM) was used as 100% baseline for complex I inhibition. decrease EC20 36
RESPIRATION 0.9 µM 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Oligomycin A (1µM) was used as 100% baseline for complex II inhibition. decrease EC20 36
SWELLING > 200 µM 30 mins mouse liver mitochondria swelling assay: Absorbance at 545 nm using a fluorescence multi-well plate reader (CaCl2 (50 µM) was considered as the 100% baseline for the swelling ) increase EC20 36

Target Dose Time Species Model Method Action Positive criterion Reference
NADH:ubiquinone reductase < 50 µM 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Rotenone (2µM) was used as 100% baseline for complex I inhibition. inhibit EC20 36
Succinate dehydrogenase 0.9 µM 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Oligomycin A (1µM) was used as 100% baseline for complex II inhibition. inhibit EC20 36
Cytochrome c > 200 µM 30 mins mouse liver mitochondria Cytochrome c release was evaluated using ELISA kit ( 20 µg/ml Alamethicin was used as 100% baseline) release EC20 36

Organism Test type Route Dose (normalized dose) Effect Source
man LDLo oral 29mg/kg (29mg/kg) Annals of Emergency Medicine. Vol. 16, Pg. 702, 1987.
pigeon LDLo intradermal 100mg/kg (100mg/kg) "Abdernalden's Handbuch der Biologischen Arbeitsmethoden." Vol. 4, Pg. 1306, 1935.
dog LDLo oral 10mg/kg (10mg/kg) "Abdernalden's Handbuch der Biologischen Arbeitsmethoden." Vol. 4, Pg. 1306, 1935.
man LDLo oral 286mg/kg (286mg/kg) Journal of Toxicology, Clinical Toxicology. Vol. 29, Pg. 45, 1991.
man LDLo oral 114mg/kg (114mg/kg) Human & Experimental Toxicology. Vol. 18, Pg. 640, 1999.
women TDLo oral 549mg/kg (549mg/kg) Japanese Journal of Acute Medicine. Vol. 20, Pg. 1557, 1996.
rat LD50 intraperitoneal 871mg/kg (871mg/kg) Gigiena Truda i Professional'nye Zabolevaniya. Labor Hygiene and Occupational Diseases. Vol. 19(3), Pg. 30, 1975.
mouse LD50 intravenous 10700ug/kg (10.7mg/kg) Proceedings of the Society for Experimental Biology and Medicine. Vol. 78, Pg. 392, 1951.
rat LD50 oral 14600ug/kg (14.6mg/kg) Gigiena i Sanitariya. For English translation, see HYSAAV. Vol. 52(1), Pg. 21, 1987.
dog LDLo intradermal 2mg/kg (2mg/kg) "Abdernalden's Handbuch der Biologischen Arbeitsmethoden." Vol. 4, Pg. 1306, 1935.
chicken LDLo intradermal 13mg/kg (13mg/kg) "Abdernalden's Handbuch der Biologischen Arbeitsmethoden." Vol. 4, Pg. 1306, 1935.
man LDLo oral 2857mg/kg (2857mg/kg) Journal of Toxicology, Clinical Toxicology. Vol. 29, Pg. 131, 1991.
rabbit LDLo intravenous 10560ug/kg (10.56mg/kg) Biochemische Zeitschrift. Vol. 70, Pg. 144, 1915.
man LDLo unreported 2941ug/kg (2.941mg/kg) "Poisoning; Toxicology, Symptoms, Treatments," 2nd ed., Arena, J.M., Springfield, IL, C.C. Thomas, 1970Vol. 2, Pg. 73, 1970.
cattle LDLo oral 30mg/kg (30mg/kg) "Abdernalden's Handbuch der Biologischen Arbeitsmethoden." Vol. 4, Pg. 1306, 1935.
mouse LD50 subcutaneous 9800ug/kg (9.8mg/kg) Proceedings of the Society for Experimental Biology and Medicine. Vol. 78, Pg. 392, 1951.
rat LDLo subcutaneous 8mg/kg (8mg/kg) skin and appendages (skin): corrosive: after topical exposure Journal of Pharmacology and Experimental Therapeutics. Vol. 19, Pg. 337, 1922.
human LDLo oral 1429ug/kg (1.429mg/kg) Yakkyoku. Pharmacy. Vol. 31, Pg. 1247, 1980.
women TDLo oral 20mg/kg (20mg/kg) International Archives of Occupational and Environmental Health. Vol. 68, Pg. 342, 1996.
rat LDLo unreported 8mg/kg (8mg/kg) Biochemische Zeitschrift. Vol. 184, Pg. 360, 1927.
mouse LD50 oral 31500ug/kg (31.5mg/kg) Zhonghua Yufangyixue Zazhi. Chinese Journal of Preventive Medicine. Vol. 14, Pg. 86, 1980.
rabbit LD50 oral 20190ug/kg (20.19mg/kg) Zhonghua Yufangyixue Zazhi. Chinese Journal of Preventive Medicine. Vol. 22, Pg. 284, 1988.
man TDLo oral 14857ug/kg (14.857mg/kg) Journal of Toxicology, Clinical Toxicology. Vol. 36, Pg. 27, 1998.
man LDLo oral 123mg/kg (123mg/kg) Journal of Forensic Sciences. Vol. 36, Pg. 1163, 1992.
women TDLo oral 100mg/kg (100mg/kg) Journal of Toxicology, Clinical Toxicology. Vol. 38, Pg. 471, 2000.


  • AKOS015903780 Arsenic(III) oxide, 99.995% trace metals basis Arsenic(III) oxide, ACS reagent (primary standard)
    Arsenic(III) oxide, ReagentPlus(R), >=99.0% Arsenic(III) oxide, SAJ first grade, >=99.0% Arsenic(III) oxide, certified reference material for titrimetry, certified by BAM, according to ISO 17025, >99.5%
    Arsenic(III) oxide, p.a., 99.0% Arsenic(III) oxide, primary standard Arsenic(III) oxide, puriss. p.a., ACS reagent, 99.95-100.05% (RT)
    DB01169 IKWTVSLWAPBBKU-UHFFFAOYSA-N J-006219
    MFCD00003433 NSC92859 TR-004471
    arsenic(iii)oxide,arsenic trioxide,arsenous acid anhydride,arsenous acid,arsenic sesquioxide,white arsenic

    DrugBank Name Arsenic trioxide
    DrugBank DB01169
    CAS Number 1327-53-3
    PubChem Compound 261004
    KEGG Compound ID C13619
    KEGG Drug D02106
    PubChem.Substance 46506448
    ChEBI 30621
    PharmGKB PA448486
    ChemSpider 229103
    TTD DNC000255
    Wikipedia Arsenic_trioxide
    DPD 3812

    1. Dykens et al. (2007)