Molecular Weight(MW): 417.5
CP-673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM in cell-free assays, exhibits >450-fold selectivity over other angiogenic receptors, has antiangiogenic and antitumor activity.
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Pharmacological inhibition of PDGFR-β by cp673451 significantly attenuated the mRNA expression of BCL2A1 (E) and SERPINE (F) in ASCs.
Stem Cells 2014 10.1002/stem.1865. CP-673451 purchased from Selleck.
Selective inhibitor of PDGFR-beta CP-673451 blocked the angiogenesis of PDGFR-beta/PAE cells. The angiogenesis of PDGFR-beta/PAE cells was evaluated in the absence or presence of different concentration of PDGFR-beta specific inhibitor CP-673451, as indicated for 6 h. The concentration of CP-673451 used in this study was much lower than that required for causing a toxic effect on the cells, and specifically inhibits only the kinase activity of PDGFR-beta (Roberts et al., 2005). The network formations were visualized by Calcein-AM staining. Representative microscopic fields are shown.
Environ Toxicol Pharmacol, 2016, 46:168-73.. CP-673451 purchased from Selleck.
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|Description||CP-673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM in cell-free assays, exhibits >450-fold selectivity over other angiogenic receptors, has antiangiogenic and antitumor activity.|
CP 673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM, exhibits >450-fold selectivity over other angiogenic receptors. In glioblastoma tumors, CP-673451 (33 mg/kg) provides >50% inhibition of PDGFR-β receptor for 4 hours corresponding to an EC50 of 120 ng/mL in plasma at Cmax. In a sponge angiogenesis model, CP-673451 inhibits 70% of PDGF-BB-stimulated angiogenesis at a dose of 3 mg/kg (q.d. ×5, p.o., corresponding to 5.5 ng/mL at Cmax). CP-673451 decreases cell proliferation rate through mechanisms involving reduced phosphorylation of GSK-3α and GSK-3β. In both RD and RUCH2 cultures, CP-673451 impairs rhabdosphere-forming capacity and cell differentiation, causes increased senescence. 
|In vivo||CP 673451 (once-daily p.o. ?0 days dosing routinely) inhibits tumor growth (ED50 < 33 mg/kg) in a number of human tumor xenografts grown s.c. in athymic mice, including H460 human lung carcinoma, Colo205 and LS174T human colon carcinomas, and U87MG human glioblastoma multiforme.  In RUCH2 xenograft-bearing mice, CP 673451 reduces tumor growth and stromal cell infiltration. |
Kinase inhibition assay:A glutathione S-transferase-tagged kinase domain construct of the intracellular portion of the PDGFR-β (amino acids 693-1401, accession no. J03278) is expressed in Sf-9 cells (baculovirus expression system). Enzyme kinetics are determined by incubating the enzyme with increasing concentrations of ATP in phosphorylation buffer [50 mmol/L HEPES (pH 7.3), 125 mmol/L NaCl, 24 mmol/L MgCl2 in Nunc Immuno MaxiSorp 96-well plates previously coated with 100 μL of 100 μg/mL poly-Glu-Tyr (4:1 ratio) diluted in PBS. After 10 minutes, the plates are washed (PBS, 0.1% Tween 20), incubated with anti-phosphotyrosine-horseradish peroxidase antibody, and diluted in PBS, 0.05% Tween 20, 3% BSA for 30 minutes at room temperature. The plates are washed as above and incubated with 3,3',5,5'-tetramethylbenzidine. The reaction is stopped by adding an equal volume of 0.09 NaH2SO4. The phosphotyrosine-dependent signal is then quantitated on a plate reader at 450 nm. For routine enzyme assays, the enzyme is incubated with 10 μM ( final) ATP in the presence of compound diluted in DMSO (1.6% v/v DMSO assay final) for 30 minutes at room temperature in plates, as above, previously coated with 100 μL of 6.25 μg/mL poly-Glu-Tyr. The remainder of the assay is carried out as above, and IC50 values are calculated as percent inhibition of control.
|In vitro||DMSO||28 mg/mL warmed (67.06 mM)|
|Ethanol||4 mg/mL (9.58 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG 400+5% propylene glycol+1% Tween 80+ddH2O
For best results, use promptly after mixing.
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Frequently Asked Questions
I need to formulate CP-673451 for animal studies via oral gavage, any suggestions?
For oral gavage, S1536 CP-673451 can be dissolved in 30% PEG 400+5% propylene glycol+1% Tween 80+ddH2O at 30 mg/ml as a suspension. When preparing the solution, please add PEG 400 and propylene glycol to the compound first. Sonicate or stir it, then add Tween 80, after they mixed well, then dilute with water.