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Please be aware that this old REACH registration data factsheet is no longer maintained; it remains frozen as of 19th May 2023.

The new ECHA CHEM database has been released by ECHA, and it now contains all REACH registration data. There are more details on the transition of ECHA's published data to ECHA CHEM here.

Diss Factsheets

Toxicological information

Additional toxicological data

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Administrative data

Endpoint:
additional toxicological information
Type of information:
experimental study
Adequacy of study:
supporting study
Reliability:
2 (reliable with restrictions)
Rationale for reliability incl. deficiencies:
other: well documented and scientifically acceptable

Data source

Reference
Title:
No information
Author:
Jochheim CM et al. (2002). Glutathione-dependent metabolism|of the antitumor agent Sulofenur. Evidence for the formation|of p-chlorophenylisocyanate as a reactive intermediate.|Chem. Res. Toxicol. 15, 240-248

Materials and methods

Type of study / information:
Metabolism of the antitumor agent sulofenur. Evidence for the formation of p-chlorophenyl isocyanate as a reactive intermediate
Principles of method if other than guideline:
glutathione and N-acetylcysteine conjugates of p-chlorophenyl isocyanate excreted into bile and urine after an ip dose of sulofenur to rats were examined by mass spectrometry and combined liquid chromatography-tandem mass spectrometry
GLP compliance:
no

Test material

Constituent 1
Chemical structure
Reference substance name:
4-chlorophenyl isocyanate
EC Number:
203-176-9
EC Name:
4-chlorophenyl isocyanate
Cas Number:
104-12-1
Molecular formula:
C7H4ClNO
IUPAC Name:
1-chloro-4-isocyanatobenzene
Details on test material:
solufenur (>99% pure) was synthesized at Eli Lilly & Co.

Results and discussion

Any other information on results incl. tables

RM-Freetext:
Sulofenur is suggested to undergo bioactivation in vivo to the reactive p-chlorophenyl isocyanate which, in turn, is
trapped in the form of GSH adduct and processed further to the corresponding N-acetyl-L-cysteine conjugate.

Applicant's summary and conclusion

Executive summary:

Sulofenur is suggested to undergo bioactivation in vivo to the reactive p-chlorophenyl isocyanate which, in turn, is
trapped in the form of GSH adduct and processed further to the corresponding N-acetyl-L-cysteine conjugate.

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