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AG 18

Cat. No. M2021
AG 18 Structure
Synonym:

RG-50810;Tyrphostin 23;tyrA23;Tyrphostin A23

Size Price Availability Quantity
10mg USD 60  USD60 In stock
50mg USD 200  USD200 In stock
100mg USD 330  USD330 In stock
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Quality Control & Documentation
Biological Activity

AG 18 (Tyrphostin 23) is an inhibitor of epidermal growth factor receptor (EGFR) and platelet-derived growth factor receptor (PDGFR) kinase with IC50 values of 35 and 25 μM respectively. AG 18 inhibits EGF-stimulated cell proliferation. AG 18 also acts as a mitochondrial uncoupler that alters phosphorylation-dependent cell signaling. AG18 increased the rate of oxygen consumption and reduced cellular ATP by approximately 90% in the absence of the muscarinic agonist carbachol. AG 18 (10 μM) decreases the potency of 5-HT 4-fold and reduces the maximal contraction to 5-HT in the carotid artery. AG18 blocked parotid phosphorylation events only at concentrations that reduced ATP content. AG18 (RG-50810) also activated AMPK and/or uncoupled mitochondria in PC12, HeLa, and HEK293 cells.

Chemical Information
Molecular Weight 186.17
Formula C10H6N2O2
CAS Number 118409-57-7
Solubility (25°C) DMSO ≥ 25 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] Soltoff SP. J Biol Chem. Evidence that tyrphostins AG10 and AG18 are mitochondrial uncouplers that alter phosphorylation-dependent cell signaling.

[2] Gazit A, et al. J Med Chem. Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors.

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Keywords: AG 18, RG-50810;Tyrphostin 23;tyrA23;Tyrphostin A23 supplier, EGFR/HER2, inhibitors, activators


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