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Neocarzinostatin

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Name

Neocarzinostatin

EINECS N/A
CAS No. 9014-02-2 Density 1.52g/cm3
PSA 174.77000 LogP 1.85820
Solubility N/A Melting Point 260° (dec)
Formula C35H35NO12 Boiling Point 900.5°C at 760 mmHg
Molecular Weight 661.6519 Flash Point 498.4°C
Transport Information N/A Appearance N/A
Safety A deadly poison by ingestion, intraperitoneal, subcutaneous, and intravenous routes. An experimental teratogen. Experimental reproductive effects. Human mutation data reported. When heated to decomposition it emits acrid smoke and irritating fumes. Risk Codes N/A
Molecular Structure Molecular Structure of 9014-02-2 (NEOCARZINOSTATIN) Hazard Symbols N/A
Synonyms

Zinostatinum;Neocarzinostatin;

 

Neocarzinostatin Chemical Properties

Chemistry informtion about  Neocarzinostatin (9014-02-2) is:
Synonyms: a8544527g1 ; neocarcinostatin ; neocarzinostatink ; neocarzinostatin from streptomyces carzinostaticus ; NSC-157365
MF:C35H33NO12
Storage temp. :2-8°C
Following is the molecular structure of  Neocarzinostatin (9014-02-2) is:

Neocarzinostatin Uses

 Neocarzinostatin (9014-02-2) can be used as a medicine, and in Japan only it has been used against liver cancer clinically.

Neocarzinostatin Toxicity Data With Reference

Organism

Test

Type

Route

Reported Dose

(Normalized Dose)

Effect

Source

dog

LDLo

intraperitoneal

1mg/kg (1mg/kg)

Behavioral: somnolence (general depressed activity) behavioral: tremor gastrointestinal: nausea or vomiting

Kiso to Rinsho. Clinical Report. Vol. 10, Pg. 610, 1976.

dog

LDLo

intravenous

200ug/kg (0.2mg/kg)

Behavioral: somnolence (general depressed activity)behavioral: food intake (animal)

Kiso to Rinsho. Clinical Report. Vol. 10, Pg. 610, 1976.

mouse

LD50

intraperitoneal

1720ug/kg (1.72mg/kg)

Gastrointestinal: alteration in gastric secretion blood: changes in spleen

Journal of Antibiotics. Vol. 31, Pg. 468, 1978.

mouse

LD50

intravenous

960ug/kg (0.96mg/kg)

Behavioral: somnolence (general depressed activity) behavioral: food intake (animal) skin and appendages (skin): hair: other

Journal of Antibiotics. Vol. 28, Pg. 64, 1975.

mouse

LD50

oral

1050mg/kg (1050mg/kg)

Behavioral: somnolence (general depressed activity) behavioral: food intake (animal) skin and appendages (skin): hair: other

Journal of Antibiotics. Vol. 28, Pg. 64, 1975.

mouse

LD50

subcutaneous

7200ug/kg (7.2mg/kg)

Behavioral: altered sleep time (including change in righting reflex) gastrointestinal: "hypermotility, diarrhea" skin and appendages (skin): hair: other

Oyo Yakuri. Pharmacometrics. Vol. 11, Pg. 309, 1976.

rabbit

LD50

intravenous

900ug/kg (0.9mg/kg)

 

Journal of Antibiotics. Vol. 28, Pg. 64, 1975.

rabbit

LD50

oral

> 600mg/kg (600mg/kg)

 

Journal of Antibiotics. Vol. 28, Pg. 64, 1975.

rat

LD50

intraperitoneal

940ug/kg (0.94mg/kg)

Behavioral: altered sleep time (including change in righting reflex) gastrointestinal: "hypermotility, diarrhea" skin and appendages (skin): hair: other

Oyo Yakuri. Pharmacometrics. Vol. 11, Pg. 309, 1976.

rat

LD50

intravenous

830ug/kg (0.83mg/kg)

 

Journal of Antibiotics. Vol. 28, Pg. 64, 1975.

rat

LD50

subcutaneous

4980ug/kg (4.98mg/kg)

Behavioral: altered sleep time (including change in righting reflex) gastrointestinal: "hypermotility, diarrhea" skin and appendages (skin): hair: other

Oyo Yakuri. Pharmacometrics. Vol. 11, Pg. 309, 1976.

rat

LDLo

oral

300mg/kg (300mg/kg)

Behavioral: altered sleep time (including change in righting reflex) gastrointestinal: "hypermotility, diarrhea" skin and appendages (skin): hair: other

Oyo Yakuri. Pharmacometrics. Vol. 11, Pg. 309, 1976.

Neocarzinostatin Specification

 Neocarzinostatin (9014-02-2) is a macromolecular chromoprotein Enediyne antibiotic with anti-tumoral activity secreted by Streptomyces macromomyceticus. It consists of two parts, a labile chromophore (bicyclic dienediyne structure shown at right) and a 113 amino acid apoprotein to which the chromophore is tightly and non-covalently bound with high affinity (Kd ~ 10-10 M). The chromophore is a very potent DNA-damaging agent; it is very labile and the role of the apoprotein is to protect it and release it to the target DNA. Opening of the epoxide under reductive conditions present in cells creates favorable conditions for a Bergman_cyclization, leading to a diradical intermediate and eventually double DNA strand cleavage. Other members of the neocarzinostatin group of antibiotics are macromomycin, actinoxanthin, kedarcidin and maduropeptin.

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