DRF-1042

Product NameDRF-1042
CAS200619-13-2
MFC22H20N2O6
MW408.4
EINECS
MOL File200619-13-2.mol

Chemical Properties

Boiling point	844.6±65.0 °C(Predicted)
Density	1.53±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO: 50 mg/mL (122.43 mM)
pka	11.13±0.40(Predicted)
form	Solid
color	White to light yellow

Usage And Synthesis

Uses

DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-agent resistance (MDR) phenotype[1][2].

Biological Activity

DRF-1042 is an orally active camptothecin analog that inhibits DNA topoisomerase I (DNA topoisomerase I). DRF-1042 shows promising anticancer activity against a panel of human cancer cell lines, including multidrug resistant (MDR) phenotypes.

in vitro

DRF-1042 demonstrates superior lactone stability and good in vitro anticancer activity against a panel of human cancer cell lines including multi-drug resistance (MDR) phenotype.

in vivo

In clonogenic assay against murine, canine and human bone marrow cells, DRF-1042 treatment shows less mylosupression that supports the possibility of protracted dose schedule in both experimental and clinical studies.

target

DNA topoisomerase I

References

[1] Chatterjee A, et al. Safety, tolerability, and pharmacokinetics of a capsule formulation of DRF-1042, a novelcamptothecin analog, in refractory cancer patients in a bridging phase I study. J Clin Pharmacol. 2005 Apr;45(4):453-60. DOI:10.1177/0091270004270225
[2] Sriram Rajagopal, et al. Preclinical evaluation of the anticancer activity of DRF-1042, a novel camptothecin analog targeting Topoisomerase-I. Published April 2004.