Inhibitor SourceBook™ Second Edition

Protein Tyrosine Kinase (PTK) Inhibitors, continued
Calbiochem • Inhibitor SourceBook
Phosphorylation/Dephosphorylation
Product Cat. No. Comments Size Price
Oxindole I 499600 [3-(1H-Pyrrol-2-ylmethylene)-1,3-dihydroindol-2-one]
A potent and specific inhibitor of VEGFR kinase Flk- (IC 50 = 390 nM).
PD 53035 234490 {AG 1517; 4-[(3-Bromophenyl)amino]-6,7-dimethoxyquinazoline; Compound 32; SU 5271}
An extremely potent and specific inhibitor of EGFR kinase activity (IC 50 = 25 pM).
0 mg $64
mg $85
N InSolution PD 53035 234491 A 0 mM (500 mg/ 39 ml) solution of PD 53035 (Cat. No. 234490) in DMSO. 500 mg $85
PD 56273 513032 {6-Amino-4-[(3-bromophenyl)amino]-7-(methylamino)quinazoline}
A potent inhibitor of EGFR kinase activity (IC 50 = 690 pM).
PD 58780 513035 {4-[(3-Bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyridimine}
A potent inhibitor of the EGFR tyrosine kinase activity (80 pM). Also inhibits heregulinstimulated
autophosphorylation in SK-BR-3 (IC 50 = 49 nM) and MDA-MB-453
(IC 50 = 52 nM) breast carcinomas.
PD 68393 513033 {4-[(3-Bromophenyl)amino]-6-acrylamidoquinazoline}
A potent, cell-permeable, irreversible, and selective inhibitor of EGFR kinase activity
(IC 50 = 700 pM).
PD 74265 513040 {4-[(3-Bromophenyl)amino]-6-propionylamidoquinazoline}
A potent, cell-permeable, reversible, and selective inhibitor of EGFR kinase activity
(IC 50 = 450 pM).
PDGF Receptor Tyrosine
Kinase Inhibitor I
PDGF Receptor Tyrosine
Kinase Inhibitor II
PDGF Receptor Tyrosine
Kinase Inhibitor III
521230 [D-64406; (5-Hydroxy-1H-2-indolyl)(1H-2-indolyl)-methanone]
A cell-permeable bis( H-2-indolyl)- -methanone compound that acts as a highly
selective and ATP-competitive inhibitor of PDGFR kinase (IC 50 = 200 nM in Swiss 3T3
cells for PDGFR; 90 nM in vitro and 200 nM in PAE cells for PDGFb-R; mM for
PDGFa-R). Also reported to inhibit Fms-like tyrosine kinase 3 (Flt3) activity
(IC 50 = 300 nM for hPDGFb-R-mFlt3 and 00 nM in EOL- cells).
521231 {(5-Butanoate-1H-2-indolyl)(1H-2-indolyl)-methanone; D-65476;
[2-(1H-2-Indolylcarbonyl)-1H-5-indolyl]butanoate}
Prodrug form of Platelet Derived Growth Factor Receptor Tyrosine Kinase Inhibitor I
(Cat. No. 52 230) that acts as a highly selective, cell-permeable, ATP-competitive inhibitor
of PDGFR kinase (IC 50 = . mM, Swiss 3T3 cells). A potent inhibitor of Fms-like tyrosine
kinase 3 (Flt3) activity (IC 50 = 6.2 mM for PDGFRb-mFlt3 and 50 nM in EOL- cells).
521232 [4-(6,7-Dimethoxy-4-quinazolinyl)-N-(4-phenoxyphenyl)-1-piperazinecarboxamide]
A cell-permeable, potent, selective, ATP-competitive inhibitor of PDGF receptor family
of tyrosine kinases (IC 50 = 50 nM for a-PDGFR; 80 nM for b-PDGFR; 50 nM for c-Kit;
230 nM for Flt3).
Piceatannol 527948 (trans-3,3´,4,5´-Tetrahydroxystilbene)
Inhibitor of p72 Syk , a non-receptor tyrosine kinase (IC 50 = 0 mM).
PP Analog 529579 {4-Amino-1-tert-butyl-3-(1´-naphthyl)pyrazolo[3,4-d]pyrimidine}
A potent, cell-permeable, and selective inhibitor of Src-family tyrosine kinases. Displays
high selectivity for 338G v-Src (IC 50 = .5 nM) with respect to the wild-type v-Src
(IC 50 = .0 mM). Also inhibits wild-type Fyn (IC 50 = 600 nM). Not available for sale in the
United States.
N PP Analog II, NM-
PP
529581 {4-Amino-1-tert-butyl-3-(1´-naphthylmethyl)pyrazolo[3,4-d]pyrimidine; Mutant Kinases
Inhibitor II; NM}
A cell-permeable PP analog (Cat. No. 529479) that acts as a potent and selective
ATP-competitive inhibitor of mutant kinases over wild-type (IC = 3.2 nM for T339G,
50
c-Fyn-as vs. .0 mM for c-Fyn; 4.3 nM for I338G, v-src-as vs. 28 mM for v-src; 5 nM
for F80G, CDK2-as vs. 29 mM for CDK2; 8 nM for F89G, CAMK IIa-as vs. 24 mM for
CaMKII; 20 nM for T3 5A, c-Abl-as2 vs. 3.4 mM for c-Abl). Shown to activate mutants
of Ire , a transmembrane kinase.
PP2 529573 {AG 1879; 4-Amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine}
A potent and selective inhibitor of the Src family of tyrosine kinases. Inhibits p56 lck
(IC 50 = 4 nM), p59 fynT (IC 50 = 5 nM), and Hck (IC 50 = 5 nM).
mg $ 04
500 mg $ 07
mg $ 04
mg $93
mg $ 37
mg $ 57
mg $ 05
mg $4
mg —
mg $82
mg $92
InSolution PP2 529576 A 0 mM ( mg/33 ml) solution of PP2 (Cat. No. 529573) in DMSO. mg $97
PP3 529574 (4-Amino-7-phenylpyrazol[3,4-d]pyrimidine)
A negative control compound for PP2. Shown to inhibit EGFR kinase (IC 50 = 2.7 mM).
mg $57
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