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Amrubicin

Cat. No. M3697
Amrubicin Structure
Synonym:

SM-5887

Size Price Availability
2mg USD 240  USD240 Custom Synthesis
5mg USD 450  USD450 Custom Synthesis
10mg USD 650  USD650 Custom Synthesis
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Quality Control & Documentation
Biological Activity

Amrubicin is a synthetic anthracycline which has been shown in preclinical studies to have broad-spectrum anti-tumor activity and a lower potential for cardiotoxicity as compared to doxorubicin. Amrubicin Shows Promise in Relapsed or Refractory Small Cell Lung Cancer.Amrubicin acts by inhibiting topoisomerase II, and has been compared in clinical trials with topotecan, a Topoisomerase I inhibitor.It has also been studied for the treatment of bladder carcinoma and gastric cancer. Amrubicin appears to have significant activity against invasive thymoma.

Chemical Information
Molecular Weight 483.47
Formula C25H25NO9
CAS Number 110267-81-7
Form Solid
Solubility (25°C) DMSO
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] von Pawel J, et al. J Clin Oncol. Randomized Phase III Trial of Amrubicin Versus Topotecan As Second-Line Treatment for Patients With Small-Cell Lung Cancer.

[2] Yardley DA, et al. Breast Cancer Res Treat. Amrubicin as second- or third-line treatment for women with metastatic HER2-negative breast cancer: a Sarah Cannon Research Institute phase 1/2 trial.

[3] Fukushima T, et al. Jpn J Clin Oncol. Successful salvage chemotherapy with amrubicin for invasive thymoma associated with myasthenia gravis.

[4] Higashiguchi M, et al. Anticancer Res. Long-term amrubicin chemotherapy for small-cell lung cancer.

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Keywords: Amrubicin, SM-5887 supplier, Topoisomerase, inhibitors, activators


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