INTRODUCTION

NCI Investigational Drugs - Chemical Information is designed
to provide selected relevant chemical and physical data to
investigators involved in various multidisciplinary studies of drugs
which were developed or are being developed by the
Developmental Therapeutics Program, Division of Cancer
Treatment, National Cancer Institute. Monographs are presented on
most of the investigational agents currently distributed by the
Division of Cancer Treatment for clinical study. Monographs are
also presented for many compounds in preclinical development.

Selected chemical information is presented in a standardized format
to facilitate the retrieval of specific information. The format
includes the chemical name, common names, molecular formula,
molecular weight and structure of each compound. Generally,
approximate solubility, stability, ultraviolet absorption, and
chromatographic information are provided. Occasionally other
selected data are provided (e.g., optical rotation).

The approximate solubility data are generated during the early
stages of drug development. These studies are not necessarily
conducted under "saturation conditions" and are intended only to
provide rough solubility estimates for guidance during the
formulation development process. As such, they should be useful
for providing leads such as the potential suitability of a particular
solvent as a vehicle for animal studies or for use in extracting the
drug from biological fluids.

The bulk drug stability data provided are also generated early in
the development process. These studies are intended to identify
potential stability problems as well as identify a possible storage
condition for the bulk drug. The data are not intended to support
long term stability during storage. They can, however, be used as
a general guide as to the relative stability of the bulk drug. The
solution stability data may provide guidance as to the storage of
solutions prepared from bulk drug (e.g., some solutions may need
to be prepared immediately before use).

Data from some analytical testing are presented as a range of
values. These ranges are derived from the assay of multiple bulk
drug samples and are typical of the values that were generated
from the better samples received for analysis. Unless otherwise
indicated, samples are assayed on an "as is" basis. Corrections for
water content are not generally applied.

The chromatographic procedures provided [usually high
performance liquid chromatographic (HPLC) procedures] are those
which were developed by the analytical contractors and have been
used for the assay of multiple lots of bulk drugs and clinical drug
products. As such, the methods may not be immediately useful for
other applications. For example, the inclusion of an
extraction /isolation step or a change in detection mode may be
necessary to allow the quantitation of drug in biological fluids.
However, the methods can provide a starting point for developing
these more specialized procedures, thus eliminating some of the
time spent on methods development. It should be noted that the
HPLC columns listed in the method description are the actual
columns used in our analyses of the material. This is not to imply
that other similar columns will not perform as well or, perhaps,
better. Also, it should be recognized that the transfer of HPLC
methodology from laboratory to laboratory is likely to require some
amount of "fine tuning" and that retention volumes and other
chromatographic characteristics may not be identical for a given set
of operating conditions.

Toxicity data were derived from the Registry of Toxic Effects of
Chemical Substances compiled by the National Institute of
Occupational Safety and Health, the Toxicology Branch (NCI) and
in vivo screening data (NCI). These data are provided for general
guidance only and no warranty of accuracy is implied by their
inclusion. Further information should be obtained from the primary
source.

Additional analytical chemistry information is available upon
request from the Pharmaceutical Resources Branch, National
Cancer Institute.

For information on the pharmaceutical dosage forms refer to the
companion publication NCI Investigational Drugs:
Pharmaceutical Data.

Copies of these publications or questions pertaining to the drugs
contained therein may be addressed to:

Chief, Pharmaceutical Resources Branch
Developmental Therapeutics Program
National Cancer Institute
Executive Plaza North, Room 818
Bethesda, Maryland 20892
FAX: (301)- 496 -8333