| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
PDGFRalpha kinase inhibitor 1 targets platelet-derived growth factor receptor alpha (PDGFRalpha), a type II receptor tyrosine kinase that plays a critical role in cell proliferation, migration, and survival. The compound acts as a selective inhibitor of PDGFRalpha with an IC₅0 of 132 nM. It shows significantly lower potency against PDGFRbeta (IC₅0 = 6115 nM), demonstrating approximately 46-fold selectivity for PDGFRalpha over PDGFRbeta. This high selectivity makes it a valuable tool for studying PDGFRalpha-specific signaling pathways.
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| ln Vitro |
PDGFRα kinase inhibitor 1 (CHMFL-PDGFR-159, compound 15i) has a mild inhibitory action on DDR1 kinase (IC50: 2462±126 nM) [1].
In vitro, PDGFRalpha kinase inhibitor 1 is a highly selective type II PDGFRalpha kinase inhibitor with IC₅0 values of 132 nM for PDGFRalpha and 6115 nM for PDGFRbeta. Its approximately 46-fold selectivity for PDGFRalpha over PDGFRbeta makes it a valuable tool for dissecting PDGFRalpha-specific signaling pathways. The compound's inhibitory activity is typically assessed in kinase activity assays using recombinant PDGFRalpha and PDGFRbeta enzymes. Its selectivity profile makes it useful for studying the role of PDGFRalpha in various cellular processes and diseases. |
| ln Vivo |
In vivo studies of PDGFRalpha kinase inhibitor 1 are likely focused on evaluating its efficacy in animal models of diseases where PDGFRalpha plays a role, such as fibrosis, cancer, and vascular diseases. As a highly selective PDGFRalpha inhibitor, the compound may offer advantages over less selective PDGFR inhibitors by reducing off-target effects. Further in vivo studies are needed to fully characterize its pharmacokinetic properties, bioavailability, and efficacy in various disease models.
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| Enzyme Assay |
For in vitro enzyme/receptor binding assays, PDGFRalpha kinase inhibitor 1 is evaluated using kinase activity assays that measure PDGFRalpha-mediated phosphorylation. The compound is incubated with recombinant PDGFRalpha kinase and ATP at various concentrations. Kinase activity is quantified by measuring phosphorylation of peptide substrates using radiometric, fluorescence-based, or ELISA methods. IC₅0 values are determined from dose-response curves. Selectivity profiling against PDGFRbeta and other kinases is performed to confirm specificity. Standard assay conditions include physiological buffer systems with appropriate ATP concentrations.
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| Cell Assay |
For in vitro cellular experiments, PDGFRalpha kinase inhibitor 1 is tested in cell lines expressing PDGFRalpha to evaluate its effects on receptor signaling and cellular functions. Cells are cultured in appropriate media and treated with various concentrations of the compound. PDGFRalpha phosphorylation and downstream signaling pathways (such as PI3K/AKT and MAPK/ERK) are assessed by Western blotting. Cell proliferation, migration, and survival are evaluated using standard assays. The compound's effects on PDGFRbeta-mediated signaling can be assessed in parallel to confirm selectivity.
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| Animal Protocol |
For in vivo animal experiments, PDGFRalpha kinase inhibitor 1 can be administered to animals via various routes including oral gavage, intravenous injection, or intraperitoneal injection, depending on its solubility and pharmacokinetic properties. The compound's efficacy can be evaluated in models of fibrosis, cancer, or other diseases where PDGFRalpha plays a role. Typical dosing regimens may range from 1 to 50 mg/kg. Pharmacodynamic markers such as PDGFRalpha phosphorylation are measured in tissues. Disease progression and physiological parameters are assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of PDGFRalpha kinase inhibitor 1 are not extensively detailed in the public literature. As a small molecule with a molecular weight of 586.69, it may have reasonable oral bioavailability and tissue distribution. The compound's chemical properties suggest it may be suitable for oral administration. Detailed parameters such as Cₘₐₓ, Tₘₐₓ, AUC, half-life, and clearance would need to be determined through comprehensive PK studies. The compound's metabolism and excretion pathways remain to be fully characterized.
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| Toxicity/Toxicokinetics |
Toxicological data for PDGFRalpha kinase inhibitor 1 are limited, as it is primarily a research tool. As a PDGFRalpha inhibitor, its toxicity would depend on the importance of PDGFRalpha signaling for normal cellular function. PDGFRalpha is involved in various physiological processes including development, wound healing, and tissue homeostasis. Comprehensive toxicology studies including acute and repeated-dose toxicity, genotoxicity, and cardiotoxicity assessments would be needed for further development. Appropriate safety precautions should be taken when handling this compound.
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| References | |
| Additional Infomation |
PDGFRalpha kinase inhibitor 1 is a research compound used to study PDGFRalpha signaling and develop therapies for PDGFRalpha-related diseases. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. The compound is a highly selective type II PDGFRalpha kinase inhibitor with IC₅0 values of 132 nM for PDGFRalpha and 6115 nM for PDGFRbeta.
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| Molecular Formula |
C34H34N8O2
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|---|---|
| Molecular Weight |
586.686166286469
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| Exact Mass |
586.28
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| CAS # |
2209053-93-8
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| PubChem CID |
129318936
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
44
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| Complexity |
897
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C=NC=CC=1)N(CC1C=CC(C(NC2C=CC(C)=C(C=2)NC2N=CC=C(C3C=NC=CC=3)N=2)=O)=CC=1)CCN(C)C
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| InChi Key |
NWVOHJOHQOHBMB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C34H34N8O2/c1-24-8-13-29(20-31(24)40-34-37-17-14-30(39-34)27-6-4-15-35-21-27)38-32(43)26-11-9-25(10-12-26)23-42(19-18-41(2)3)33(44)28-7-5-16-36-22-28/h4-17,20-22H,18-19,23H2,1-3H3,(H,38,43)(H,37,39,40)
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| Chemical Name |
N-[2-(dimethylamino)ethyl]-N-[[4-[[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]carbamoyl]phenyl]methyl]pyridine-3-carboxamide
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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 : ~260 mg/mL (~443.16 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (3.70 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 21.7 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: ≥ 2.17 mg/mL (3.70 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 21.7 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: ≥ 2.17 mg/mL (3.70 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 | 1.7045 mL | 8.5224 mL | 17.0448 mL | |
| 5 mM | 0.3409 mL | 1.7045 mL | 3.4090 mL | |
| 10 mM | 0.1704 mL | 0.8522 mL | 1.7045 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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