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IPI-493

Cat. No. M2776
IPI-493 Structure
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1mg USD 220  USD220 Out of stock
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Quality Control & Documentation
Biological Activity

IPI-493 is a potent and orally bioavailable HSP90 inhibitor with Ki of 21 nM.

Chemical Information
Molecular Weight 545.62
Formula C28H39N3O8
CAS Number 64202-81-9
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] Zhou Zhou, et al. Heat shock protein 90 inhibitors suppress pyroptosis in THP-1 cells

[2] Qiang Shan, et al. Physiological Functions of Heat Shock Proteins

[3] Giuseppe Floris, et al. The Novel HSP90 inhibitor, IPI-493, is highly effective in human gastrostrointestinal stromal tumor xenografts carrying heterogeneous KIT mutations

[4] Meletios-Athanassios Dimopoulos, et al. Tanespimycin as antitumor therapy

[5] Britt Erika Hanson, et al. Retaspimycin hydrochloride (IPI-504): a novel heat shock protein inhibitor as an anticancer agent

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