DRF-1042
- Product Name
- DRF-1042
- CAS No.
- 200619-13-2
- Chemical Name
- DRF-1042
- Synonyms
- DRF-1042;DRF 1042,DRF1042;(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)-;(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
- CBNumber
- CB92677375
- Molecular Formula
- C22H20N2O6
- Formula Weight
- 408.4
- MOL File
- 200619-13-2.mol
DRF-1042 Property
- 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
N-Bromosuccinimide Price
- Product number
- CS-0090380
- Product name
- DRF-1042
- Purity
- 98.04%
- Packaging
- 5mg
- Price
- $458
- Updated
- 2021/12/16
- Product number
- CS-0090380
- Product name
- DRF-1042
- Purity
- 98.04%
- Packaging
- 10mg
- Price
- $780
- Updated
- 2021/12/16
DRF-1042 Chemical Properties,Usage,Production
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.
DRF-1042 Preparation Products And Raw materials
Raw materials
Preparation Products
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