521232
PDGFR Tyrosine Kinase Inhibitor III - CAS 205254-94-0 - Calbiochem
Synonym(s):
4-(6,7-Dimethoxy-4-quinazolinyl)-N-(4-phenoxyphenyl)-1-piperazinecarboxamide
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About This Item
UNSPSC Code:
12352200
General description
A cell-permeable piperazinyl-quinazoline carboxamide compound that acts as a potent, ATP-competitive, reversible, and selective inhibitor of PDGF receptor family of tyrosine kinases (IC50 = 0.05 μM for α-PDGFR; 0.08 μM for β-PDGFR; 0.05 μM for c-Kit; 0.23 μM for Flt3). Affects the activities of other kinases only at much higher concentrations (IC50 ≥ 30 μM for EGFR, FGFR, Src, PKA & PKC). Reported to block the PDGF-BB induced proliferation of porcine aorta smooth muscle cells (IC50 = 0.25 μM).
Biochem/physiol Actions
Target IC50:0.05 μM for α-PDGFR; 0.08 μM for β-PDGFR; 0.05 μM for c-Kit; 0.23 μM for Flt3
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Storage Class
10-13 - German Storage Class 10 to 13
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Kenji Matsuno et al.
Journal of medicinal chemistry, 46(23), 4910-4925 (2003-10-31)
We have previously reported that a series of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives were potent and selective inhibitors of platelet-derived growth factor receptor (PDGFR) phosphorylation and demonstrated several biological effects such as suppression of neointima formation following balloon injury in rat carotid
Kenji Matsuno et al.
Journal of medicinal chemistry, 45(20), 4513-4523 (2002-09-20)
4-[4-(N-Substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives such as KN1022 are potent inhibitors of the phosphorylation of platelet derived growth factor receptor (PDGFR). Structure activity relationships in the (thio)urea moiety, the phenyl ring itself, the linker between these two moieties, and the piperazine moiety
Kenji Matsuno et al.
Bioorganic & medicinal chemistry letters, 13(18), 3001-3004 (2003-08-28)
Here, we investigated the structure-activity relationships of the 6,7-dimethoxyquinazoline moiety. With regard to exploration of positions and varieties of substituents on the quinazoline ring, 6,7-dialkoxy substitution was optimal. This study suggests the possibility of further modifications for this moiety.
Kenji Matsuno et al.
Journal of medicinal chemistry, 45(14), 3057-3066 (2002-06-28)
A new series of 4-[4-(N-substituted carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives were found to show potent and selective inhibition of platelet-dervied growth factor (PDGF) receptor phosphorylation. In this exploration of the structure-activity relationships (SARs) of the prototype inhibitor KN1022, the 4-nitrophenylurea moiety was probed.
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