Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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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
Synonyms | PDGFR 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 |
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Specifications & Purity | Moligand™, ≥98% |
Storage Temp | Store at 2-8°C |
Shipped In | Wet ice |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor 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). |
pKa | pKₐ: 13.18 (Predicted), pKₐ: 9.48 (Predicted) |
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IUPAC Name | 4-(6,7-dimethoxyquinazolin-4-yl)-N-(4-phenoxyphenyl)piperazine-1-carboxamide |
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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 |
PubChem CID | 10907042 |
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ChEMBL Ligand | CHEMBL102346 |
CAS Registry No. | 205254-94-0 |
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Solubility | Soluble in DMSO (10 mg/ml). |
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Refractive Index | n20D1.67 (Predicted) |
Boil Point(°C) | ~713.68° C at 760 mmHg (Predicted) |
Melt Point(°C) | 292.08° C (Predicted) |
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] |