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| | Rubitecan Chemical Properties |
| Melting point | 182-186°C | | alpha | D23 +27° (c = 0.2 in CH3OH-CHCl3, 1:4) | | Boiling point | 816.3±65.0 °C(Predicted) | | density | 1.63 | | Fp | 106℃ | | storage temp. | Sealed in dry,Room Temperature | | solubility | DMSO, Chloroform, Methanol | | form | Solid | | pka | 11.16±0.20(Predicted) | | color | Yellow | | Merck | 14,8288 | | CAS DataBase Reference | 91421-42-0(CAS DataBase Reference) |
| Safety Statements | 24/25 | | WGK Germany | 3 | | RTECS | UQ0493300 | | HS Code | 29399990 |
| | Rubitecan Usage And Synthesis |
| Description | Rubitecan, marketed by Supergen as Orathecin, is a promising oral treatment for solid melanoma, prostate, breast, ovarian, and other cancers, as well as leukemia. It is a derivative of camptothecin, a topoisomerase inhibitor known from Chinese Traditional Medicine. It selectively targets the critical S-stage of cellular reproduction – particularly in acidic environments, as in many cancer cells – relaxing DNA supercoiling and generating lethal breaks in the DNA. Due to insolubility, its biological delivery mechanism is not yet effective, and it has not been approved for clinical use.
| | Reference | https://www.sciencedirect.com/topics/medicine-and-dentistry/rubitecan
https://en.wikipedia.org/wiki/Rubitecan
https://en.wikipedia.org/wiki/Topoisomerase_inhibitor
https://en.wikipedia.org/wiki/Camptothecin#cite_note-Y.Pommier_2003-14
https://www.ncbi.nlm.nih.gov/pubmed/1995300
| | Description | Rubitecan is a DNA topoisomerase I inhibitor. It inhibits DNA topoisomerase I and increases the fraction of supercoiled DNA in a cell-free assay in a concentration-dependent manner. Rubitecan inhibits the growth of A121 ovarian and H460 lung cancer cells (IC50s = 4 and 2 nM, respectively). It also inhibits the growth of doxorubicin-susceptible and -resistant MCF-7 breast cancer cells (IC50s = 2 and 3 nM, respectively). Rubitecan (4 mg/kg twice per week) reduces tumor growth in a U937 leukemia mouse xenograft model. | | Chemical Properties | Yellow Amorphous Powder | | Uses | Semisynthetic camptothecin which inhibits DNA topoisomerase I. Prodrug of 9-aminocamptothecin. Antineoplastic. | | Definition | ChEBI: A pyranoindolizinoquinoline that is camptothecin in which the hydrogen at position 9 has been replaced by a nitro group. It is a prodrug for 9-aminocamptothecin. |
| | Rubitecan Preparation Products And Raw materials |
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