- Rubitecan USP/EP/BP
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- $1.10 / 1g
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2025-11-18
- CAS:91421-42-0
- Min. Order: 1g
- Purity: 99.9%
- Supply Ability: 100 Tons Min
- Rubitecan
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- $0.00 / 1KG
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2025-04-04
- CAS:91421-42-0
- Min. Order: 1KG
- Purity: 98%
- Supply Ability: 1Ton
- Rubitecan
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- $0.00 / 1Kg
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2020-05-03
- CAS:91421-42-0
- Min. Order: 1KG
- Purity: 99.0%
- Supply Ability: 800 ton
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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 | | pka | 11.16±0.20(Predicted) | | form | Solid | | color | Yellow | | biological source | synthetic (organic) | | Merck | 14,8288 | | InChI | InChI=1S/C20H15N3O6/c1-2-20(26)13-7-16-17-10(8-22(16)18(24)12(13)9-29-19(20)25)6-11-14(21-17)4-3-5-15(11)23(27)28/h3-7,26H,2,8-9H2,1H3/t20-/m0/s1 | | InChIKey | VHXNKPBCCMUMSW-FQEVSTJZSA-N | | SMILES | N1C2C(=C([N+]([O-])=O)C=CC=2)C=C2CN3C(C=12)=CC1[C@](CC)(O)C(=O)OCC=1C3=O | | CAS DataBase Reference | 91421-42-0(CAS DataBase Reference) |
| Safety Statements | 24/25 | | WGK Germany | 3 | | RTECS | UQ0493300 | | HS Code | 29399990 | | Storage Class | 11 - Combustible Solids |
| | 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. | | References | [1] E RUBIN. Identification of a mutant human topoisomerase I with intact catalytic activity and resistance to 9-nitro-camptothecin.[J]. The Journal of Biological Chemistry, 1994, 269 4: 2433-2439.
[2] H R HINZ. Pharmacokinetics of the in vivo and in vitro conversion of 9-nitro-20(S)-camptothecin to 9-amino-20(S)-camptothecin in humans, dogs, and mice.[J]. Cancer research, 1994, 54 12: 3096-3100.
[3] R. BERNACKI. In Vitro Antitumor Activity of 9‐Nitro‐Camptothecin as a Single Agent and in Combination with other Antitumor Drugs[J]. Annals of the New York Academy of Sciences, 2000, 922 1. DOI: 10.1111/j.1749-6632.2000.tb07046.x [4] P. PANTAZIS. 9-nitro-camptothecin delays growth of U-937 leukemia tumors in nude mice and is cytotoxic or cytostatic for human myelomonocytic leukemia lines in vitro[J]. European Journal of Haematology, 1993, 50 2: 81-89. DOI: 10.1111/j.1600-0609.1993.tb00146.x |
| | Rubitecan Preparation Products And Raw materials |
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