AG126 is a tyrosine kinase inhibitor (TKI) that can suppress the phosphorylation of ERK1 and ERK2 at 25-50 μM. AG126 can be used for meiotic, mitotic and postmitotic studies.

Physicochemical Properties

Molecular Formula	C₁₀H₅N₃O₃
Molecular Weight	215.17
Exact Mass	215.033
Elemental Analysis	C, 55.82; H, 2.34; N, 19.53; O, 22.31
CAS #	118409-62-4
Related CAS #	118409-62-4
PubChem CID	2046
Appearance	Light yellow to yellow solid powder
Density	1.5±0.1 g/cm3
Boiling Point	381.9±42.0 °C at 760 mmHg
Melting Point	184 °C
Flash Point	184.8±27.9 °C
Vapour Pressure	0.0±0.9 mmHg at 25°C
Index of Refraction	1.689
LogP	1.66
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	1
Heavy Atom Count	16
Complexity	388
Defined Atom Stereocenter Count	0
SMILES	N#C/C(C#N)=C/C1=CC=C([N+]([O-])=O)C(O)=C1
InChi Key	DUQADSPERJRQBW-UHFFFAOYSA-N
InChi Code	InChI=1S/C10H5N3O3/c11-5-8(6-12)3-7-1-2-9(13(15)16)10(14)4-7/h1-4,14H
Chemical Name	2-[(3-hydroxy-4-nitrophenyl)methylidene]propanedinitrile
Synonyms	AG 126; AG126; AG-126; UNII-7YA4AMD1JC; Tyrphostin A 10; Tyrphostin AG 126; Tyrphostin A 10; alpha-Cyano-(3-hydroxy-4-nitro)cinnamonitrile
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	ERK1/2
ln Vitro	AG126 (10 μM; overnight) increases the ARPE-19 cells' viability[2]. AG126 at concentrations greater than 10 μM , they become toxic to ARPE-19 cells and can increase the toxicity of H2O2[2]. AG126 (0.1-100 μM) blocks the growth of BRMECs that is induced by VEGF[4]
ln Vivo	AG 126 (intraperitoneal injection; 1-10 mg/kg; 1 h and 6 h after Zymosan treatment) treatment decreases the severity of multiple organ failure (MOF) brought on by Zymosan-induced peritonitis in rats[3].
Animal Protocol	Male Sprague-Dawley rats treated with Zymosan (500 mg/kg)[3] 10 mg/kg, 3 mg/kg or 1 mg/kg Intraperitoneal injection; 10, 3, or 1 mg/kg; 1 h and 6 h after Zymosan treatment
References	[1]. The tyrosine kinase inhibitor tyrphostin AG126 reduces the development of acute and chronic inflammation. Am J Pathol. 2000 Jul;157(1):145-58. [2]. Oxidative stress causes ERK phosphorylation and cell death in cultured retinal pigment epithelium: prevention of cell death by AG126 and 15-deoxy-delta 12, 14-PGJ2. BMC Ophthalmol. 2003 Mar 21;3:5. [3]. The tyrosine kinase inhibitor tyrphostin AG 126 reduces the multiple organ failure induced by zymosan in the rat. Intensive Care Med. 2002 Jun;28(6):775-88 [4]. Role for extracellular signal-responsive kinase-1 and -2 in retinal angiogenesis. Invest Ophthalmol Vis Sci. 2003 Apr;44(4):1722-31.
Additional Infomation	2-[(3-hydroxy-4-nitrophenyl)methylidene]propanedinitrile is a nitrophenol. Tyrphostin AG 126 is a member of the tyrphostin family of tyrosine kinase inhibitors, that actively blocks lipopolysaccharide-induced production of tumor necrosis factor-a and nitric oxide in macrophages. (NCI)

Solubility Data

Solubility (In Vitro)

DMSO: 43~100 mg/mL (199.9~464.8 mM) Ethanol: ~2 mg/mL (~9.3 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (11.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	4.6475 mL	23.2374 mL	46.4749 mL
	5 mM	0.9295 mL	4.6475 mL	9.2950 mL
	10 mM	0.4647 mL	2.3237 mL	4.6475 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.