Inhibitor SourceBook™ Second Edition

Protein Tyrosine Kinase (PTK) Inhibitors, continued
Calbiochem • Inhibitor SourceBook
Phosphorylation/Dephosphorylation
Product Cat. No. Comments Size Price
AG 494 658407 [a-Cyano-(3,4-dihydroxy)-N-phenylcinnamide; Tyrphostin B48]
Inhibitor of EGFR kinase autophosphorylation (IC 50 = .24 mM) that is slightly less active
than AG 555 (Cat. No. 658404).
AG 527 658402 [a-Cyano-(-)-(R)-N-(a-phenethyl)-3,4-dihydroxycinnamide; (-)-(R)-N-
(a-Methylbenzyl)-3,4-dihydroxybenzylidinecyanoacetamide; Tyrphostin B44(-)]
An inhibitor of EGFR kinase autophosphorylation (IC 50 = 2.5 mM). Also inhibits the
phosphorylation of poly-GAT by the EGF receptor (IC 50 = 400 nM).
AG 537, Bis-Tyrphostin 658418 (Bis-Tyrphostin)
Competitively inhibits EGFR kinase autophosphorylation (IC 50 = 400 nM).
AG 538 658403 [a-Cyano-(3,4-dihydroxy)cinnamoyl-(3´,4´-dihydroxyphenyl)ketone; Tyrphostin AG 538]
A potent, competitive inhibitor of insulin-like growth factor- receptor (IGF- R)
kinase autophosphorylation (IC 50 = 400 nM). Also inhibits the phosphorylation of PTK
substrate poly (Glu,Tyr) by IGF- R, IR, EGF-R, and Src (IC 50 = 60 nM, 3 nM, and 2.4 mM
respectively).
I-OMe-AG 538 658417 [a-Cyano-(3-methoxy,4-hydroxy,5-iodo)cinnamoyl-(3´,4´-dihydroxyphenyl)ketone;
Tyrphostin I-OMe-AG 538]
An analog of AG 538 (Cat. No. 658403) that acts as an inhibitor of IGF- receptor kinase
both in vitro and in intact cells. Inhibition is competitive with respect to the substrate
binding site of IGF- receptor kinase. Exhibits enhanced cell-permeability and increased
resistance to oxidation.
AG 555 658404 [a-Cyano-(3,4-dihydroxy)-N-(3-phenylpropyl)cinnamide; Tyrphostin B46]
A potent inhibitor of EGFR kinase autophosphorylation (IC 50 = 700 nM). Exhibits opposite
potency profiles with AG 527 (Cat. No. 658402) for EGF receptor autophosphorylation
versus poly-GAT substrate phosphorylation.
AG 556 658415 [a-Cyano-(3,4-dihydroxy)-N-(4-phenylbutyl)cinnamide; Tyrphostin B56]
A selective inhibitor of EGFR kinase (IC 50 = 5 mM) over HER -2 kinase autophosphorylation.
AG 592 658406 {AGL 2592; 2-Cyano-N-(4-{4-[2-cyano-3-(3,4-dihydroxyphenyl)-acryloylamino]cyclohexylmethyl}-cyclohexyl)-3-(3,4-dihydroxyphenyl)-acrylamide}
A selective, cell-permeable inhibitor of EGFR-tyrosine kinase activity (IC 50 = 20.3 mM).
Blocks thymidine uptake in HER- 4 cells, and displays anti-proliferative properties.
AG 825 121765 [4-Hydroxy-3-methoxy-5-(benzothiazolylthiomethyl)benzylidenecyanoacetamide]
A potent, selective and ATP-competitive inhibitor of HER-2 (neu/erbB-2, IC 50 = 350 nM)
relative to HER- (IC 50 = 9 mM) autophosphorylation.
AG 835 658409 [a-Cyano-(+)-(S)-N-(a-phenethyl)-(3,4-dihydroxy)cinnamide; Tyrphostin B50(+)]
A less active enantiomer of AG 527 (Cat. No. 658402) that inhibits EGFR kinase
poly-GAT (poly-Glu-Ala-Tyr) substrate phosphorylation (IC 50 = 860 nM).
AG 879 658460 [a-Cyano-(3,5-di-t-butyl-4-hydroxy)thiocinnamide]
An inhibitor of nerve growth factor-dependent pp 40 c-trk tyrosine phosphorylation
(EC 50 = 0 mM). Does not affect the tyrosine phosphorylation of EGFR or PDGFR.
AG 957 121761 [4-Amino-N-(2,5-dihydroxybenzyl)methyl benzoate; NSC 654705]
A potent and selective inhibitor of human p2 0 brc-abl (K i = 750 nM) over p 40 bcr-abl
(K i = 0 mM).
AG 957, Adamantyl
Ester
121762 [4-Amino-N-(2,5-dihydroxybenzyl)adamantyl Benzoate; 4-(2,5-Dihydroxybenzylamino)benzoic
Acid Adamantan-1-yl Ester]
A lipophilic, adamantyl ester form of tyrphostin AG 957 (Cat. No. 2 76 ) that displays
anti-proliferative properties. Shown to be selective and ~3-4 fold more potent than
AG 957 as a bcr/abl kinase inhibitor, and also exhibits a longer serum half-life in vivo.
AG 024 121767 (3-Bromo-5-t-butyl-4-hydroxy-benzylidenemalonitrile)
A specific inhibitor of insulin-like growth factor- (IGF- ) and insulin receptor kinases
with significantly lower IC 50 values for IGF- than for insulin receptors.
AG 295 658550 (6,7-Dimethyl-2-phenylquinoxaline)
A selective inhibitor of PDGFR kinase (IC 50 = 500 nM). Does not affect EGFR
autophosphorylation.
5 mg $32
5 mg $33
5 mg $69
5 mg $67
5 mg $67
5 mg $33
5 mg $32
5 mg $ 78
2 mg $93
5 mg $32
5 mg $90
5 mg $92
5 mg $ 84
mg $67
5 mg $87
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