AG-1478 (Tyrphostin AG-1478) is a highly potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor with an IC50 of 3 nM. AG-1478 (Tyrphostin AG-1478) reversibly prevents rat brain Kv1.5 potassium channels (IC50 = 9.8 mM) independent of PTK activity. Additionally, AG-1478 (Tyrphostin AG-1478) also suppresses the growth of leiomyoma and myometrium cell cultures with IC50 values of 5.6 and 5.7 mM, respectively. AG-1478 (Tyrphostin AG-1478) blocke the activation of MAP kinase and strongly represses induction of fos gene expression and DNA synthesis. AG-1478 (Tyrphostin AG-1478) blocks G3 enhanced effects on cell apoptosis.
Aging (Albany NY). 2020 Oct 28;12(20):20801-20816.
Synergistic effect between LH and estrogen in the acceleration of cumulus expansion via GPR30 and EGFR pathways
AG-1478 purchased from AbMole
|Source||Aging (Albany NY) (2020), Figure 5, AG-1478 (AbMole Bioscience, TX, USA)|
|Cell Lines||cumulus cells|
|Incubation Time||8 h|
|Results||The mRNA of GPR30 was downregulated by EGF stimulation, while AG1478 reversed the inhibition of GPR30 transcription caused by EGF treatment|
|Source||Aging (Albany NY) (2020), Figure 4, AG-1478 (AbMole Bioscience, TX, USA)|
|Concentrations||1 mg/kg body weight|
|Incubation Time||1, 3, 5, and 7 day|
|Results||The results showed that hCG significantly activated p-EGFR (Tyr1068), but AG1478 blocked the activation of p-EGFR induced by hCG stimulation|
|Source||Sci Rep (2018). Figure 4. AG-1478|
|Cell Lines||corneal endothelial cells|
|Incubation Time||7 days|
|Results||The addition of TGF-β1 (with or without AG-1478) also generated the expression of n-cadherin at the cell membrane. The gain of n-cadherin expression following addition of TGF-β1 was confirmed using western blotting|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 25 mg/mL|
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