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AG 18

Cat. No. M2021
AG 18 Structure
Synonym:

RG-50810, Tyrphostin 23

Size Price Availability Quantity
10mg USD 70 In stock
50mg USD 250 In stock
100mg USD 380 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 186.17
Formula C10H6N2O2
CAS Number 118409-57-7
Purity >99%
Solubility DMSO
Storage at -20°C
References

Evidence that tyrphostins AG10 and AG18 are mitochondrial uncouplers that alter phosphorylation-dependent cell signaling.
Soltoff SP. J Biol Chem. 2004 Mar 19;279(12):10910-8. PMID: 14688271.

Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors.
Gazit A, et al. J Med Chem. 1989 Oct;32(10):2344-52. PMID: 2552117.

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Keywords: AG 18, RG-50810, Tyrphostin 23 supplier, EGFR/HER2, inhibitors

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