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PDGFR Tyrosine Kinase Inhibitor III - ≥98%, high purity , CAS No.205254-94-0, Inhibitor of platelet derived growth factor receptor beta

  • Moligand™
  • ≥98%
Item Number
P338497
Grouped product items
SKUSizeAvailabilityPrice Qty
P338497-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$47.90
P338497-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$119.90
P338497-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$189.90
P338497-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$439.90
P338497-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$639.90
P338497-100mg
100mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$909.90

an ATP-competitive PDGFR inhibitor

Basic Description

SynonymsPDGFR Tyrosine Kinase Inhibitor III|PDGF Receptor Tyrosine Kinase Inhibitor III|205254-94-0|4-(6,7-dimethoxyquinazolin-4-yl)-N-(4-phenoxyphenyl)piperazine-1-carboxamide|CHEMBL102346|1-Piperazinecarboxamide, 4-(6,7-dimethoxy-4-quinazolinyl)-N-(4-phenoxyphe
Specifications & PurityMoligand™, ≥98%
Storage TempStore at 2-8°C
Shipped InWet ice
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of platelet derived growth factor receptor beta
Product Description

PDGFR Tyrosine Kinase Inhibitor III is a cell-permeable, potent, selective, and ATP-competitive inhibitor of the PDGFR family of tyrosine kinases (IC|50|= 50 nM for PDGFR-α, 80 nM for PDGFR-β, 50 nM for c-Kit, and 230 nM for Flt-3/Flk-2). PDGFR Tyrosine Kinase Inhibitor III inhibits the activities of other kinases only at much higher concentrations (IC50 > 30μM for EGFR, FGFR, Src, PKA, and PKC). Reported to block PDGF-BB-induced proliferation of porcine aorta smooth muscle cells (IC|50|= 250 nM).

Product Properties

pKapKₐ: 13.18 (Predicted), pKₐ: 9.48 (Predicted)

Associated Targets

CDK1 Tchem Cyclin-dependent kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ERBB4 Tclin Receptor tyrosine-protein kinase erbB-4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EPHA1 Tchem Ephrin type-A receptor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FAM124A Tdark Protein FAM124A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EGFR Tclin Epidermal growth factor receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SRC Tclin Proto-oncogene tyrosine-protein kinase Src 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FLT4 Tclin Vascular endothelial growth factor receptor 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

YES1 Tclin Tyrosine-protein kinase Yes 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR1 Tclin Fibroblast growth factor receptor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR2 Tclin Fibroblast growth factor receptor 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MET Tclin Hepatocyte growth factor receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

IGF1R Tclin Insulin-like growth factor 1 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

JAK3 Tclin Tyrosine-protein kinase JAK3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MERTK Tchem Tyrosine-protein kinase Mer 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIM1 Tchem Serine/threonine-protein kinase pim-1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PDGFRA Tclin Platelet-derived growth factor receptor alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIM2 Tchem Serine/threonine-protein kinase pim-2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIM3 Tchem Serine/threonine-protein kinase pim-3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

RPS6KA2 Tchem Ribosomal protein S6 kinase alpha-2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKCE Tchem Protein kinase C epsilon type 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKCH Tchem Protein kinase C eta type 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKD1 Tchem Serine/threonine-protein kinase D1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BTK Tclin Tyrosine-protein kinase BTK 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKB Tchem Aurora kinase B 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKC Tchem Aurora kinase C 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FLT1 Tclin Vascular endothelial growth factor receptor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KDR Tclin Vascular endothelial growth factor receptor 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TNK2 Tclin Activated CDC42 kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AKT3 Tchem RAC-gamma serine/threonine-protein kinase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AKT2 Tchem RAC-beta serine/threonine-protein kinase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AKT1 Tchem RAC-alpha serine/threonine-protein kinase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHEK1 Tchem Serine/threonine-protein kinase Chk1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CLK3 Tchem Dual specificity protein kinase CLK3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CLK2 Tchem Dual specificity protein kinase CLK2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3A Tclin Glycogen synthase kinase-3 alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KIT Tclin Mast/stem cell growth factor receptor Kit 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

NTRK1 Tclin High affinity nerve growth factor receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

JAK2 Tclin Tyrosine-protein kinase JAK2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MTOR Tclin Serine/threonine-protein kinase mTOR 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 4-(6,7-dimethoxyquinazolin-4-yl)-N-(4-phenoxyphenyl)piperazine-1-carboxamide
INCHI InChI=1S/C27H27N5O4/c1-34-24-16-22-23(17-25(24)35-2)28-18-29-26(22)31-12-14-32(15-13-31)27(33)30-19-8-10-21(11-9-19)36-20-6-4-3-5-7-20/h3-11,16-18H,12-15H2,1-2H3,(H,30,33)
InChi Key INTPTKHSGKBHHW-UHFFFAOYSA-N
Canonical SMILES COC1=C(C=C2C(=C1)C(=NC=N2)N3CCN(CC3)C(=O)NC4=CC=C(C=C4)OC5=CC=CC=C5)OC
Isomeric SMILES COC1=C(C=C2C(=C1)C(=NC=N2)N3CCN(CC3)C(=O)NC4=CC=C(C=C4)OC5=CC=CC=C5)OC
PubChem CID 10907042
Molecular Weight 485.53

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilitySoluble in DMSO (10 mg/ml).
Refractive Indexn20D1.67 (Predicted)
Boil Point(°C)~713.68° C at 760 mmHg (Predicted)
Melt Point(°C)292.08° C (Predicted)

Related Documents

References

1. Matsuno K, Ushiki J, Seishi T, Ichimura M, Giese NA, Yu JC, Takahashi S, Oda S, Nomoto Y.  (2003)  Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 3. Replacement of quinazoline moiety and improvement of metabolic polymorphism of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives..  J Med Chem,  46  (23): (4910-25).  [PMID:14584942]

Solution Calculators