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Tyrphostin RG 13022

Cat. No. M8818
Tyrphostin RG 13022 Structure
Synonym:

RG13022

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25mg USD 237  USD237 4-7 Days
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Quality Control & Documentation
Biological Activity

RG13022 is a non-phenolic tyrphostin-class tyrosine kinase inhibitor. RG13022 inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM. RG13022 inhibits colony formation and DNA synthesis by HER 14 cells, which were stimulated by 50 ng/mL EGF, in a dose-dependent manner. The IC50s are 1 and 3 μM for HER 14 colony formation and DNA synthesis, respectively. RG-13022 also totally blocks estrogen-stimulated phosphorylation of the EGF receptor, as well as estrogen-induced cell proliferation, suggesting that functioning TK pathways are required for estrogen action.

In vivo, RG13022 suppresses tumor growth in nude mice. RG13022 also increases the life span of these tumor-bearing nude mice.

Chemical Information
Molecular Weight 266.29
Formula C16H14N2O2
CAS Number 136831-48-6
Solubility (25°C) Soluble in DMSO
Soluble in ethanol
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] T Yoneda, et al. Cancer Res. The antiproliferative effects of tyrosine kinase inhibitors tyrphostins on a human squamous cell carcinoma in vitro and in nude mice

[2] K B Reddy, et al. Cancer Res. Inhibition of breast cancer cell growth in vitro by a tyrosine kinase inhibitor

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