JNJ-10198409
Based on 1 publication(s) in Google Scholar
JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM).
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- Pureza: 99.58%
- No. CAS: 627518-40-5
- Fòrmula: C18H16FN3O2
- Peso molecular:325.34
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Kinase Inhibitor Library
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Publications Citing Use of MedChemExpress (MCE) JNJ-10198409
More
Actividad biológica
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PDGFRβ 4.2 nM (IC50) |
PDGFRα 45 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
0.007 μM
Compound: 17, JNJ-10198409
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Antiproliferative activity against human melanoma tumor cell line A375
Antiproliferative activity against human melanoma tumor cell line A375
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[PMID: 16366598] |
| ASPC1 | IC50 |
0.592 μM
Compound: 17, JNJ-10198409
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Antiproliferative activity against human pancreatic tumor cell line AsPC1
Antiproliferative activity against human pancreatic tumor cell line AsPC1
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[PMID: 16366598] |
| HUVEC | IC50 |
4.87 μM
Compound: 17, JNJ-10198409
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Antiproliferative activity against LSGS stimulated HUVEC
Antiproliferative activity against LSGS stimulated HUVEC
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[PMID: 16366598] |
| LNCaP | IC50 |
0.009 μM
Compound: 17, JNJ-10198409
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Antiproliferative activity against human prostate tumor cell line LnCAP
Antiproliferative activity against human prostate tumor cell line LnCAP
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[PMID: 16366598] |
| LoVo | IC50 |
0.017 μM
Compound: 17, JNJ-10198409
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Antiproliferative activity against human colon tumor cell line LoVo
Antiproliferative activity against human colon tumor cell line LoVo
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[PMID: 16366598] |
| NCI-H460 | IC50 |
0.01 μM
Compound: 17, JNJ-10198409
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Antiproliferative activity against human lung tumor cell line H460
Antiproliferative activity against human lung tumor cell line H460
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[PMID: 16366598] |
| PC-3 | IC50 |
0.027 μM
Compound: 17, JNJ-10198409
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Antiproliferative activity against human prostate tumor cell line PC3
Antiproliferative activity against human prostate tumor cell line PC3
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[PMID: 16366598] |
| T47D | IC50 |
0.032 μM
Compound: 17, JNJ-10198409
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Antiproliferative activity against human breast tumor cell line T47D
Antiproliferative activity against human breast tumor cell line T47D
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[PMID: 16366598] |
| U-87MG ATCC | IC50 |
13 μM
Compound: 17, JNJ-10198409
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Antiproliferative activity against human glioma tumor cell line U87MG
Antiproliferative activity against human glioma tumor cell line U87MG
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[PMID: 16366598] |
Chemical Information
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No. CAS 627518-40-5
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Appearance Solid
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Peso molecular 325.34
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Fòrmula C18H16FN3O2
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Color Light yellow to yellow
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SMILES
COC1=CC2=C(C=C1OC)CC3=C2NN=C3NC4=CC=CC(F)=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Stem Cells Int
Endothelial Cells Promote Migration of Mesenchymal Stem Cells via PDGF-BB/PDGFR β-Src-Akt in the Context of Inflammatory Microenvironment upon Bone Defect. [Abstract]2022 Sep 24:2022:2401693. PMID: 36193255
Solvente y solubilidad
DMSO : 83.33 mg/mL (256.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. D'Andrea MR, et al. Validation of in vivo pharmacodynamic activity of a novel PDGF receptor tyrosine kinase inhibitor using immunohistochemistry and quantitative image analysis. Mol Cancer Ther. 2005 Aug;4(8):1198-204. [Content Brief]
[2]. Ho CY, et al. (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells. J Med Chem. 2005 Dec 29;48(26):8163-73. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0737 mL | 15.3685 mL | 30.7371 mL | 76.8427 mL |
| 5 mM | 0.6147 mL | 3.0737 mL | 6.1474 mL | 15.3685 mL | |
| 10 mM | 0.3074 mL | 1.5369 mL | 3.0737 mL | 7.6843 mL | |
| 15 mM | 0.2049 mL | 1.0246 mL | 2.0491 mL | 5.1228 mL | |
| 20 mM | 0.1537 mL | 0.7684 mL | 1.5369 mL | 3.8421 mL | |
| 25 mM | 0.1229 mL | 0.6147 mL | 1.2295 mL | 3.0737 mL | |
| 30 mM | 0.1025 mL | 0.5123 mL | 1.0246 mL | 2.5614 mL | |
| 40 mM | 0.0768 mL | 0.3842 mL | 0.7684 mL | 1.9211 mL | |
| 50 mM | 0.0615 mL | 0.3074 mL | 0.6147 mL | 1.5369 mL | |
| 60 mM | 0.0512 mL | 0.2561 mL | 0.5123 mL | 1.2807 mL | |
| 80 mM | 0.0384 mL | 0.1921 mL | 0.3842 mL | 0.9605 mL | |
| 100 mM | 0.0307 mL | 0.1537 mL | 0.3074 mL | 0.7684 mL |
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