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Lurtotecan

Cat. No. M28541
Lurtotecan Structure
Synonym:

GI147211; OSI-211

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Biological Activity

Lurtotecan (GI147211; OSI-211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan has anticancer effects.

Chemical Information
Molecular Weight 518.56
Formula C28H30N4O6
CAS Number 149882-10-0
Form Solid
Solubility (25°C) DMSO 4.33 mg/mL (ultrasonic)
Storage -20°C, protect from light, dry, sealed
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] Graham G Dark, et al. J Clin Oncol. Randomized trial of two intravenous schedules of the topoisomerase I inhibitor liposomal lurtotecan in women with relapsed epithelial ovarian cancer: a trial of the national cancer institute of Canada clinical trials group

[2] Michael V Seiden, et al. Gynecol Oncol. A phase II study of liposomal lurtotecan (OSI-211) in patients with topotecan resistant ovarian cancer

[3] Francis J Giles, et al. Cancer. Phase I and pharmacokinetic study of a low-clearance, unilamellar liposomal formulation of lurtotecan, a topoisomerase 1 inhibitor, in patients with advanced leukemia

[4] Diederik F S Kehrer, et al. J Clin Oncol. Phase I and pharmacologic study of liposomal lurtotecan, NX 211: urinary excretion predicts hematologic toxicity

[5] J P Desjardins, et al. Anticancer Drugs. Biodistribution of NX211, liposomal lurtotecan, in tumor-bearing mice

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  Catalog
Abmole Inhibitor Catalog




Keywords: Lurtotecan, GI147211; OSI-211 supplier, Topoisomerase, inhibitors, activators


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