| Identification | Back Directory | [Name]
DRF-1042 | [CAS]
200619-13-2 | [Synonyms]
DRF-1042
(4S)-4-Ethyl-4-hydroxy-12-(2-hydroxyethoxy)-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
1H-Pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione, 4-ethyl-4-hydroxy-12-(2-hydroxyethoxy)-, (4S)- | [Molecular Formula]
C22H20N2O6 | [MDL Number]
MFCD11983152 | [MOL File]
200619-13-2.mol | [Molecular Weight]
408.4 |
| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
11.13±0.40(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [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]
| [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. |
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