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Rubitecan

Cat. No. M20696
Rubitecan Structure
Synonym:

9-NC, 9-Nitro-camptothecin, Partaject Orathecin, Partaject rubitecan, RFS 2000

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Quality Control & Documentation
Biological Activity

Rubitecan is a topoisomerase I inhibitor extracted from the bark and leaves of the Camptotheca acuminata tree, which is native to China. Rubitecan is an oral camptothecin with antitumour activity.

Chemical Information
Molecular Weight 393.35
Formula C20H15N3O6
CAS Number 91421-42-0
Solubility (25°C) DMSO 58 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jeffrey W Clark. Expert Opin Investig Drugs. Rubitecan

[2] No authors listed. Drugs R D. Rubitecan: 9-NC, 9-Nitro-20(S)-camptothecin, 9-nitro-camptothecin, 9-nitrocamptothecin, RFS 2000, RFS2000

[3] P M Fracasso, et al. Ann Oncol. Phase I study of rubitecan and gemcitabine in patients with advanced malignancies

[4] Howard Sands, et al. Anticancer Drugs. Preclinical activity of an i.v. formulation of rubitecan in IDD-P against human solid tumor xenografts

[5] Beppino C Giovanella, et al. Int J Oncol. Preclinical evaluation of the anticancer activity and toxicity of 9-nitro-20(S)-camptothecin (Rubitecan)

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Keywords: Rubitecan, 9-NC, 9-Nitro-camptothecin, Partaject Orathecin, Partaject rubitecan, RFS 2000 supplier, Topoisomerase, inhibitors, activators

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