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AG 555

Cat. No. M20583
AG 555 Structure
Synonym:

Tyrphostin B46

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Biological Activity

AG-555 is an inhibitor of tyrosine kinase , interacts directly with topoisomerase I, thus preventing DNA relaxation. It inhibits EGFR with an IC50 of 0.7 μM.

Chemical Information
Molecular Weight 322.36
Formula C19H18N2O3
CAS Number 133550-34-2
Solubility (25°C) DMSO 64 mg/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] I Seri, et al. Int J Oncol. Tyrphostin AG-555 inhibits early and late stages of Moloney murine leukemia virus replication cycle

[2] Kang Xia, et al. J Agric Food Chem. Analysis of cyromazine in poultry feed using the QuEChERS method coupled with LC-MS/MS

[3] Sabine Baars, et al. J Biol Chem. Tyrphostin AG 555 inhibits bovine papillomavirus transcription by changing the ratio between E2 transactivator/repressor function

[4] H Ben-Bassat, et al. Cancer Res. Inhibitors of epidermal growth factor receptor kinase and of cyclin-dependent kinase 2 activation induce growth arrest, differentiation, and apoptosis of human papilloma virus 16-immortalized human keratinocytes

[5] N Osherov, et al. FEBS Lett. Tyrphostin AG 494 blocks Cdk2 activation

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Keywords: AG 555, Tyrphostin B46 supplier, EGFR/HER2, inhibitors, activators


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