JNJ-10198409 |
رقم الكتالوجGC14544
One-Click Copy Product Info
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JNJ-10198409 هو مثبط انتقائي نسبيًا ، نشط عن طريق الفم ، ومثبط PDGF-RTK (مستقبل عامل النمو مشتق من الصفائح الدموية التيروزين كيناز) ATP (IC50 = 2 نانومتر)إنه عامل مضاد لتكاثر الخلايا الورمية ومضاد لتولد الأوعيةJNJ-10198409 له نشاط جيد ضد PDGFR-كيناز (IC50 = 4.2 نانومتر) و PDGFR-α كيناز (IC50 = 45 نانومتر)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 627518-40-5
Sample solution is provided at 25 µL, 10mM.
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JNJ-10198409 is a small molecule inhibitor of platelet-derived growth factor (PDGF-BB) tyrosine kinase [1].
Platelet-derived growth factor (PDGF) is a ubiquitous mitogen involved in regulating cell growth and division, embryonic development, cell proliferation, cell migration, and angiogenesis. Overexpression of PDGF has been associated with several diseases such as atherosclerosis, fibrotic disorders and malignancies. Inhibition of the tyrosine kinase activity of growth factor receptors such as the platelet-derived growth factor (PDGF-BB) receptor can have potent antiangiogenic and antiproliferative activity. Recombinant PDGF is used in medicine to help heal chronic ulcers and in orthopedic surgery and periodontistry to treat bone loss [2].
In human coronary artery smooth muscle cells, JNJ-10198409 inhibited the activity of platelet-derived growth factor (PDGF-BB) tyrosine kinase with an IC50 value of 4.2 nM when tested. JNJ-10198409 was a competitive antagonist of the ATP binding and hydrolysis at PDGF-BB receptor, resulting in a dose dependent inhibition of tumor growth and angiogenesis [1].
References:
[1] Ho C Y, Ludovici D W, Maharoof U S M, 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]. Journal of medicinal chemistry, 2005, 48(26): 8163-8173.
[2] Raines E W, Bowen-Pope D F, Ross R. Platelet-derived growth factor[M]//Peptide growth factors and their receptors I. Springer Berlin Heidelberg, 1990: 173-262.
| Cas No. | 627518-40-5 | SDF | |
| Chemical Name | (Z)-N-(6,7-dimethoxy-1,2-dihydroindeno[1,2-c]pyrazol-3(4H)-ylidene)-3-fluoroaniline | ||
| Canonical SMILES | COC1=C(OC)C=C2C(CC3=C2NN/C3=N\C4=CC=CC(F)=C4)=C1 | ||
| Formula | C18H16FN3O2 | M.Wt | 325.34 |
| الذوبان | ≤10mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0737 mL | 15.3685 mL | 30.7371 mL |
| 5 mM | 614.7 μL | 3.0737 mL | 6.1474 mL |
| 10 mM | 307.4 μL | 1.5369 mL | 3.0737 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >97.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)