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| | DRF-1042 Basic information |
| Product Name: | DRF-1042 | | 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)-;DRF 1042,DRF1042;(4S)-4-Ethyl-4-hydroxy-12-(2-hydroxyethoxy)-1,12-dihydro-14H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H)-dione;(4S)-4-Ethyl-4-hydroxy-12-(2-hydroxyethoxy)-1,12-dihydro-14H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H)-dione | | CAS: | 200619-13-2 | | MF: | C22H20N2O6 | | MW: | 408.4 | | EINECS: | | | Product Categories: | | | Mol File: | 200619-13-2.mol |  |
| | DRF-1042 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 |
| | DRF-1042 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 | | | 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. |
| | DRF-1042 Preparation Products And Raw materials |
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