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ABT-869 (Linifanib) is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of the vascular endothelial growth factor (VEGF) and platelet derived growth factor (PDGF) receptor families. ABT-869 (Linifanib) showed potent antiproliferative and apoptotic properties in vitro and in animal cancer xenograft models. The kinase inhibition profile of ABT-869 is evident in cellular assays of RTK phosphorylation (IC₅₀ values of 2, 4 and 7 nM for PDGFRβ, KDR and CSF-1R, respectively) and VEGF-stimulated proliferation (0.2 nM IC₅₀ for human endothelial cells). ABT-869 is active in advanced non-small cell lung cancer as second- or third-line therapy. Increased adverse event rates were observed at the high dose of linifanib.
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Source | Oral Oncol (2013). Figure 4. ABT-869 |
| Method | Analysis of apoptosis | |
| Cell Lines | SCC-22A and B cells | |
| Concentrations | 20 μM | |
| Incubation Time | 12 h | |
| Results | ABT-869 treatment increased the apoptotic population by 4.61 and 3.11-fold and by 9.15 and 5.33-fold increase in combination in SCC-22A and B cells, as compared to untreated and radiation alone groups respectively |
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Source | Oral Oncol (2013). Figure 3. ABT-869 |
| Method | Cell cycle analysis | |
| Cell Lines | SCC-22A and B cells | |
| Concentrations | 20 μM | |
| Incubation Time | 12 h | |
| Results | Compared to control group, we observed significant accumulation in G2/M phase in SCC-22A (42.2% versus 23.4% in control) and in SCC-22B cells (24.6% versus 17% in control), after ABT-869 treatment, indicating that a higher number of cells were blocked in a more radiosensitive phase of the cell cycle. |
| Cell Experiment | |
|---|---|
| Cell lines | HUAEC cells |
| Preparation method | Cell Proliferation. HUAEC were plated into 96-well plates at 2,500 per well and incubated with serum-free medium for 24 hours. Drug and VEGF (final, 10 ng/mL) were added and incubated for 72 hours in serum-free medium. For carcinoma cell lines, 2,500 per well were plated overnight in full growth medium. Drug was added to the cells in full growth medium and incubated for 72 hours. For leukemia cells, generally 50,000 per well were plated in full growth medium, drug added, and incubated for 72 hours. The effects on proliferation were determined by addition of Alamar Blue (final solution, 10%), incubation for 4 hours at 37°C in a CO2 incubator, and analysis in a fluorescence plate reader (544 nm, excitation: 590 nm, emission). For VEGF-stimulated growth, percent inhibition of proliferation was determined using the difference between VEGF-stimulated cells and unstimulated cells as the control, and IC50 values were determined by nonlinear regression analysis of the concentration response data. |
| Concentrations | 0~1µM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | HT1080 (A), H526 (B), and MX-1 (C) human tumor cells xenograft models |
| Formulation | 2% ethanol, 5% Tween 80, 20% PEG400, 73% saline |
| Dosages | 1.5, 5 or 15mg/kg bid |
| Administration | orally |
| Molecular Weight | 375.41 |
| Formula | C21H18FN5O |
| CAS Number | 796967-16-3 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| SU5208
SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2). |
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| (Z)-Orantinib
(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. |
| (Rac)-SAR131675
(Rac)-SAR131675 is the racemate of SAR131675. |
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