| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
The compound primarily targets the platelet-derived growth factor receptor (PDGFR) family of tyrosine kinases. It exhibits IC50 values of 0.05 µM for α-PDGFR, 0.08 µM for β-PDGFR, 0.05 µM for c-Kit, and 0.23 µM for Flt3. It is an inhibitor of tyrosine kinases FLT3, PDGFR, and KIT. By inhibiting these kinases, it blocks downstream signaling pathways involved in cell proliferation, migration, and survival. Its ATP-competitive nature means it competes with ATP for binding to the kinase domain.
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| ln Vitro |
In vitro, PDGF Receptor Tyrosine Kinase Inhibitor III is a potent inhibitor of PDGFR, EGFR, FGFR, PKA, and PKC. Its activity is characterized by its ability to inhibit receptor phosphorylation and downstream signaling in cells expressing these kinases. The compound's IC50 values for α-PDGFR (0.05 µM), β-PDGFR (0.08 µM), c-Kit (0.05 µM), and Flt3 (0.23 µM) demonstrate its potent inhibitory activity. It is a multikinase inhibitor with a broad spectrum of activity.
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| ln Vivo |
In vivo, PDGF Receptor Tyrosine Kinase Inhibitor III has been used in research on amyotrophic lateral sclerosis (ALS). Its ability to inhibit multiple kinases makes it a valuable tool for studying the role of these signaling pathways in various diseases, including cancer and neurodegenerative disorders. Specific in vivo efficacy data, including dosing regimens and disease models, is not detailed in the provided search results. Further studies are needed to fully characterize its in vivo activity and therapeutic potential.
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| Enzyme Assay |
The in vitro activity of PDGF Receptor Tyrosine Kinase Inhibitor III is assessed using cell-free kinase activity assays. Recombinant kinases (PDGFRα, PDGFRβ, c-Kit, Flt3, EGFR, FGFR, PKA, PKC) are incubated with a substrate peptide and ATP in the presence of varying concentrations of the compound. The phosphorylation of the substrate is measured, typically using a radioactive (e.g., [γ-³²P]ATP) or fluorescence-based method. The IC50 is determined from dose-response curves. For selectivity profiling, the compound is tested against a panel of kinases to assess its specificity.
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| Cell Assay |
For cellular assays, cells expressing PDGFR, EGFR, FGFR, or other target kinases are cultured in appropriate media. Cells are treated with various concentrations of PDGF Receptor Tyrosine Kinase Inhibitor III (typically 0.01-10 µM) for defined periods (1-24 hours). The phosphorylation of the target kinases and their downstream signaling molecules (e.g., Akt, ERK) is analyzed by Western blotting using phospho-specific antibodies. Cell proliferation is assessed using MTT or CellTiter-Glo assays. Cell migration and invasion are assessed using Transwell chambers.
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| Animal Protocol |
In vivo, PDGF Receptor Tyrosine Kinase Inhibitor III is typically administered orally or intraperitoneally to animal models. In ALS models, the compound is administered at various doses, and disease progression is assessed by measuring motor function, survival, and histopathological changes in the spinal cord. In cancer models, the compound is administered to mice bearing tumor xenografts, and tumor growth is monitored. Pharmacodynamic studies involve measuring the phosphorylation of target kinases in tumor or tissue samples.
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| ADME/Pharmacokinetics |
PDGF Receptor Tyrosine Kinase Inhibitor III has a molecular weight of 485.53 g/mol and a molecular formula of C27H27N5O4. It is soluble in DMSO at 90 mg/mL. The compound should be stored as a powder at -20°C (stable for 3 years) or at 4°C (stable for 2 years). Specific pharmacokinetic parameters such as bioavailability, half-life, and volume of distribution are not detailed in the provided search results.
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| Toxicity/Toxicokinetics |
Specific toxicity data for PDGF Receptor Tyrosine Kinase Inhibitor III is not available in the provided search results. As a multikinase inhibitor, it may affect normal cellular processes that depend on the inhibited kinases, potentially leading to side effects such as myelosuppression, gastrointestinal effects, or skin rash. The compound is intended for research purposes only and is not approved for human or veterinary use. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
PDGF receptor tyrosine kinase inhibitor III is an N-arylpiperazine compound with the structure piperazine, wherein the hydrogen atom at position 1 of the nitrogen atom is replaced by a (4-phenoxyphenyl)aminocarbonyl group, and the hydrogen atom at position 4 of the nitrogen atom is replaced by a 6,7-dimethoxyquinazoline-4-yl group. It is an inhibitor of tyrosine kinases FLT3, PDGFR, and KIT, belonging to EC 2.7.10.1 (receptor protein tyrosine kinase) inhibitors. It is an N-arylpiperazine, N-carbamoylpiperazine, aromatic ether, phenylurea compound, quinazoline compound, and tertiary amine compound.
PDGF Receptor Tyrosine Kinase Inhibitor III is a research compound that has been developed as a potent and selective inhibitor of the PDGF receptor family of tyrosine kinases. It is a multikinase inhibitor that also targets EGFR, FGFR, PKA, and PKC. The compound is used as a tool to study the role of PDGFR and other kinases in cell proliferation, migration, and survival. It has been investigated in research on amyotrophic lateral sclerosis. PDGF Receptor Tyrosine Kinase Inhibitor III is not approved for clinical use and is intended for research purposes only. |
| Molecular Formula |
C27H27N5O4
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|---|---|
| Molecular Weight |
485.544
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| Exact Mass |
485.206
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| Elemental Analysis |
C, 66.79; H, 5.61; N, 14.42; O, 13.18
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| CAS # |
205254-94-0
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| Related CAS # |
205254-94-0
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| PubChem CID |
10907042
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| Appearance |
White to off-white solid powder
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| LogP |
4.869
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
36
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| Complexity |
692
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(N1CCN(C2=C3C=C(OC)C(OC)=CC3=NC=N2)CC1)NC4=CC=C(OC5=CC=CC=C5)C=C4
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| InChi Key |
INTPTKHSGKBHHW-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
4-(6,7-dimethoxyquinazolin-4-yl)-N-(4-phenoxyphenyl)piperazine-1-carboxamide
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| Synonyms |
PDGF Receptor Tyrosine Kinase Inhibitor III; PDGFR Tyrosine Kinase Inhibitor III; IUN54940; IUN 54940; IUN-54940; GTPL6019; GTPL6019; GTPL-6019
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~206 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (3.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (3.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0596 mL | 10.2978 mL | 20.5956 mL | |
| 5 mM | 0.4119 mL | 2.0596 mL | 4.1191 mL | |
| 10 mM | 0.2060 mL | 1.0298 mL | 2.0596 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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