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118409-57-7 (AG 18)



AG 18 AG 18
Name AG 18
Formula C10H6N2O2
MW 186.17
CAS No. 118409-57-7
Smiles OC1=C(O)C=CC(/C=C(C#N)C#N)=C1
Synonyms 2-(3,4-Dihydroxybenzylidene)malononitrile; AG 18; AG 18 (pharmaceutical); RG 50810; RG 50858; TX 825; Tyrphostin 23; Tyrphostin A 23; Tyrphostin AG 18; 2-(3,4-dihydroxybenzylidene)malononitrile
InChI InChI=1S/C10H6N2O2/c11-5-8(6-12)3-7-1-2-9(13)10(14)4-7/h1-4,13-14H


AG-18(RG-50810; Tyrphostin A23) inhibits EGFR with IC50 of 40 μM. IC50 Value: 40 uM (inhibition of EGFR autophosphorylation)[1] Target: EGFR AG-18 (Tyrphostin A23) are inhibitors of tyrosine kinases and function by binding to the active sites of the enzymes.

Background Information

AG-18(RG-50810; Tyrphostin A23) inhibits EGFR with IC50 of 40 μM. IC50 Value: 40 uM (inhibition of EGFR autophosphorylation)[1] Target: EGFR AG-18 (Tyrphostin A23) are inhibitors of tyrosine kinases and function by binding to the active sites of the enzymes. Molecular modeling of tyrphostin A23 into the tyrosine-binding pocket in mu2 provides a structural explanation for A23 being able to inhibit the interaction between YXXPhi motifs and mu2. in vitro: A23 inhibited the internalization of (125)I-transferrin in Heb7a cells without having any discernible effect on the morphology of compartments of the endocytic pathway. Control tyrphostins, active as inhibitors of tyrosine kinase activity, but incapable of inhibiting the YXXPhi motif/mu2 interaction, did not inhibit endocytosis [2]. Tyrphostin A23 inhibits Tfn internalization and redistributes most of hTfR to the plasma membrane [3]. TK-inhibiting A23 reversibly increased membrane conductance under conditions designed to minimize Na+, Ca2+, K+, and Na+-K+ pump currents [4]. in vivo: Pretreatment with the tyrosine kinase inhibitor Tyr-23 (50 microM, 10 min) caused a slow 40% increase in baseline [Ca(2+)](i). Tyr-23 attenuated peak and plateau responses to NE, both by approximately 70%. In the absence of extracellular Ca(2+) (0 Ca), Tyr-23 reduced the immediate [Ca(2+)](i) response to NE by approximately 60%, indicative of mobilization of internal stores, and abolished the plateau phase [5]. Clinical trial: ......by MedChemexpress Co., Ltd.
AG-18 inhibits EGFR with IC50 of 35 μM. ......by Selleck Chemicals LLC
AG-18(RG-50810; Tyrphostin A23) inhibits EGFR with IC50 of 35 μM. ......by Target Molecule Corp.

Protocol(Only for Reference)

Cell Experiment

Cell lines GH3 cells
Conditions 10 μM; 0.5 hour
Method GH3 cells are plated at 5 × 104 cells/well in media containing 2% charcoal-stripped FCS and various concentrations of ghrelin, desoctanoylated ghrelin and PMA or EGF for 72 hours with the addition of 2 μCi/well [3H]thymidine for a further 6 hours. A time-course of 24 hours, 48 hours and 72 hours is performed for ghrelin stimulation and 72 hours is selected for further experiments. Studies are also performed to investigate the effect of rat ghrelin or desoctanoyl ghrelin-induced proliferation and the effect of U0126, GF109203X, AG 18, wortmannin and H-89 upon ghrelin-induced MAPK stimulation. AG 18 at 10 μM is added 30 min before each treatment. Cells are harvested before counting in the presence of scintillation fluid using a Microbeta 1450 bcounter. Experiments are repeated at least three times.
Source Selleck Chemicals LLC

Animal Experiment


Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000015211

Storage condition


DMSO by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 37 mg/mL (198.74 mM); Ethanol37 mg/mL (198.74 mM); Water<1 mg/mL (<1 mM) by Selleck Chemicals LLC

Mechanism and Indication

Signaling Pathways JAK/STAT Signaling Protein Tyrosine Kinase/RTK
Target EGFR
Research Area Cancer

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
AG 18 - No Development Reported

Safety Data of AG 18

WGKGermany : 3

Spectral Information


Suppliers List

Company Price and Availability Country/Region
Abcam 50mg/USD235() USA
Cayman Chemical Company 5mg/USD27() USA
Clearsynth Labs Limited 25mg/USD120() India
EMD Millipore 5mg/USD59() USA
Labinova AB Europe
MedChemexpress Co., Ltd. 10mg/USD50(In stock);50mg/USD215(In stock) USA
Santa Cruz Biotechnology, Inc. 10mg/USD71() USA
Selleck Chemicals LLC 10mg/USD70(In stock);10mM/1mLIn DMSO/USD90(In stock);10mM(in 1mL DMSO)/USD113(in 1mL DMSO);50mg/USD270(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD60(In stock);50mg/USD240(In stock) China
Sigma-Aldrich, Inc. 5mg/USD92() USA
Target Molecule Corp. 10mg/USD65();25mg/USD113();50mg/USD209() USA
Tocris Bioscience Inc. 10mg/USD129() USA

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Other Forms of 118409-57-7

Name CAS No Formula MW

Recommended Compounds in EGFR

Name CAS No Formula MW
Ginsenoside Rh2 78214-33-2 C36H62O8 622.87
Mutated EGFR-IN-1 1421372-66-8 C25H31N7O 445.56
AZD-9291 (mesylate) 1421373-66-1 C29H37N7O5S 595.71
Mutant EGFR inhibitor 1421373-62-7 C27H30ClN7O2 520.03
AZD-9291 1421373-65-0 C28H33N7O2 499.61
WHI-P180 (hydrochloride) 153437-55-9 C16H16ClN3O3 333.77
WHI-P180 211555-08-7 C16H15N3O3 297.31
Gefitinib (hydrochloride) 184475-55-6 C22H25Cl2FN4O3 483.36
Erlotinib (mesylate) 248594-19-6 C23H27N3O7S 489.54
BGB-102 807640-87-5 C22H25BrN4O2 457.36
Poziotinib 1092364-38-9 C23H21Cl2FN4O3 491.34
CO-1686 (hydrobromide) 1446700-26-0 C27H29BrF3N7O3 636.46
CO-1686 1374640-70-6 C27H28F3N7O3 555.55
CNX-2006 1375465-09-0 C26H27F4N7O2 545.53
PD 168393 194423-15-9 C17H13BrN4O 369.22
Afatinib (dimaleate) 850140-73-7 C32H33ClFN5O11 718.08
Chrysophanic acid 481-74-3 C15H10O4 254.24
AG-1478 153436-53-4 C16H14ClN3O2 315.75
Mubritinib 366017-09-6 C25H23F3N4O2 468.47
AST-1306 (TsOH) 1050500-29-2 C31H26ClFN4O5S 621.08

Recommended Compounds in Same Indication

Name CAS No Formula MW

Route of Synthesis




More Information

AG 18

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