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Karenitecin

Cat. No. M13742
Karenitecin Structure
Synonym:

Cositecan; BNP 1350

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Biological Activity

Karenitecin (Cositecan) is a topoisomerase I inhibitor, with potent anti-cancer activity.

Chemical Information
Molecular Weight 448.59
CAS Number 203923-89-1
Solubility (25°C) DMSO 3.03 mg/mL (ultrasonic and warming and heat to 60°C)
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] Deepika Rajesh, et al. J Neurol Neuromedicine. Karenitecin (bnp1350) and flavopridol as radiosensitizers in malignant glioma

[2] Shijie Yao, et al. Cancer Chemother Pharmacol. Stabilization of the Karenitecin® lactone by alpha-1 acid glycoprotein

[3] Pamela N Munster, et al. Expert Opin Investig Drugs. Preclinical and clinical activity of the topoisomerase I inhibitor, karenitecin, in melanoma

[4] Stuart A Grossman, et al. Neuro Oncol. Phase I and pharmacokinetic study of karenitecin in patients with recurrent malignant gliomas

[5] Eufemia Jacob, et al. Pediatr Blood Cancer. Synergy of karenitecin and mafosfamide in pediatric leukemia, medulloblastoma, and neuroblastoma cell lines

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Keywords: Karenitecin, Cositecan; BNP 1350 supplier, Topoisomerase, inhibitors, activators


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