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Alvespimycin

Cat. No. M30126
Alvespimycin Structure
Synonym:

17-DMAG; NSC 707545

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Quality Control & Documentation
Biological Activity

Alvespimycin (17-DMAG) is a potent inhibitor of Hsp90, binding to Hsp90 with an EC50 of 62 ± 29 nM.

Chemical Information
Molecular Weight 616.75
Formula C32H48N4O8
CAS Number 467214-20-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Raquel Alves, et al. Molecules. Alvespimycin Inhibits Heat Shock Protein 90 and Overcomes Imatinib Resistance in Chronic Myeloid Leukemia Cell Lines

[2] Zhou Zhou, et al. Biochem J. Heat shock protein 90 inhibitors suppress pyroptosis in THP-1 cells

[3] Yafang Hu, et al. Cancer Biol Ther. The HSP90 inhibitor alvespimycin enhances the potency of telomerase inhibition by imetelstat in human osteosarcoma

[4] Kornelius Schulze, et al. Nat Genet. Exome sequencing of hepatocellular carcinomas identifies new mutational signatures and potential therapeutic targets

[5] Zhe-Yi Hu, et al. Br J Pharmacol. A physiologically based pharmacokinetic model of alvespimycin in mice and extrapolation to rats and humans

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Keywords: Alvespimycin, 17-DMAG; NSC 707545 supplier, HSP, inhibitors, activators


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