Phenylacetic acid mustard

Phenylacetic acid mustard is the major metabolite of the cancer chemotherapeutic agent Chlorambucil (HY-13593). Chlorambucil is an alkylating agent with antitumor activity[1].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> DNA Alkylator/Crosslinker

IC50: metabolite of Chlorambucil[1]

Phenylacetic acid mustard (intraperitoneal injection; 0-20 mg/kg; 15 days) shows consistently 1.8-1.9 times greater antitumour potency thanCHL, it exhibits an ED15 value of 8.0 mg/kg[2]. Phenylacetic acid mustard (intraperitoneal injection; 0-20 mg/kg; single dose) cause 50% lethality at the dose 15.9 mg/kg[2]. Animal Model: Inbred male C3H/He mice[1] Dosage: 0 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg Administration: Intraperitoneal injection; 15 days Result: Exhibited anti-tumor activities in vivo.

[1]. Toni Pettersson-Fernholm, et al. Reactions of 4-bis(2-chloroethyl)aminophenylacetic acid (phenylacetic acid mustard) in physiological solutions.

[2]. F Y Lee, et al. Pharmacokinetic basis for the comparative antitumour activity and toxicity of chlorambucil, phenylacetic acid mustard and, -difluorochlorambucil (CB 7103) in mice.

DATA ITEMS CITED :

11

MOLECULAR FORMULA :

C12-H15-Cl2-N-O2

MOLECULAR WEIGHT :

276.18

WISWESSER LINE NOTATION :

QV1R DN2G2G

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

15 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

15900 ug/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

DOSE :

10 mg/kg

SEX/DURATION :

female 14 day(s) pre-mating

TOXIC EFFECTS :

Reproductive - Maternal Effects - ovaries, fallopian tubes Reproductive - Maternal Effects - ovaries, fallopian tubes

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

8 mg/kg

SEX/DURATION :

male 14 day(s) pre-mating

TOXIC EFFECTS :

Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands

TYPE OF TEST :

Sex chromosome loss and nondisjunction

TYPE OF TEST :

Sex chromosome loss and nondisjunction

MUTATION DATA

TYPE OF TEST :

DNA damage

TEST SYSTEM :

Rodent - hamster Fibroblast

DOSE/DURATION :

1500 umol/L

REFERENCE :

BEXBAN Bulletin of Experimental Biology and Medicine (English Translation). Translation of BEBMAE. (Plenum Pub. Corp., 233 Spring St., New York, NY 10013) V.41- 1956- Volume(issue)/page/year: 92,943,1981