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Tyrphostin 51

Cat. No. M8827
Tyrphostin 51 Structure
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Biological Activity

Tyrphostin 51 is an EGFR tyrosine kinase inhibitor.

Chemical Information
Molecular Weight 268.23
Formula C13H8N4O3
CAS Number 126433-07-6
Solubility (25°C) DMSO: soluble 5 mg of Tyrphostin 51 in 0.1 mL
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] Masahiro Ikeda, et al. Inhibitory effect of tyrphostin 47 on Shiga toxin-induced cell death

[2] Shah M Khan, et al. Epidermal growth factor receptor inhibition by tyrphostin 51 induces apoptosis in luteinized granulosa cells

[3] Jane C J Chao, et al. Effects of epidermal growth factor and its signal transduction inhibitors on apoptosis in human colorectal cancer cells

[4] M R Nichols, et al. Tyrosine kinase-independent inhibition of cyclic-AMP phosphodiesterase by genistein and tyrphostin 51

[5] A P Majumdar, et al. Inhibition of gastric mucosal regeneration by tyrphostin: evaluation of the role of epidermal growth factor receptor tyrosine kinase

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