[CAS NO. 627518-40-5] JNJ-10198409
PRODUCTS SPECIFICATIONS [627518-40-5]
DESCRIPTION [627518-40-5]
Overview
| MDL | MFCD11045292 |
|---|---|
| Molecular Weight | 325.34 |
| Molecular Formula | C18H16FN3O2 |
| SMILES | COC1=CC2=C(C=C1OC)CC3=C2NN=C3NC4=CC=CC(F)=C4 |
1 Publications Citing Use of MCE
Summary
JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor ( IC 50 =2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase ( IC 50 =4.2 nM) and PDGFR-α kinase ( IC 50 =45 nM) [1] [2] .
IC50 & Target
|
PDGFRβ 4.2 nM (IC 50 ) |
PDGFRα 45 nM (IC 50 ) |
In Vitro
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 83.33 mg/mL ( 256.13 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.0737 mL | 15.3685 mL | 30.7371 mL |
| 5 mM | 0.6147 mL | 3.0737 mL | 6.1474 mL |
| 10 mM | 0.3074 mL | 1.5369 mL | 3.0737 mL |
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1.
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2.
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
References
- [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.
- [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.