CP-673451

Catalog No.S1536

CP-673451 Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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3 Customer Reviews

  • 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.

    A549 and H1299 cells were incubated with CP-673451 in the presence of serum for 48 hours. The nuclei were stained with Hoechst, and analyzed using a fluorescent microscope. The representative images are shown.

    Onco Targets Ther 2014 7, 1215-21. 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.

Purity & Quality Control

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Biological Activity

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.
Targets
PDGFRβ [1]
(Cell-free assay)
PDGFRα [1]
(Cell-free assay)
1 nM 10 nM
In vitro

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).[1] 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. [2]

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. [1] In RUCH2 xenograft-bearing mice, CP 673451 reduces tumor growth and stromal cell infiltration. [2]

Protocol

Kinase Assay:[1]
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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.
Cell Research:[1]
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  • Cell lines: PAE
  • Concentrations: ~3000 nM
  • Incubation Time: 18 min
  • Method: PAE cells stably expressing full-length PDGFR and VEGFR have been generated. For cell-based selectivity assays, PAE cells are transfected with fulllength human PDGFR-a, PDGFR-h, or VEGFR-2. Cells are seeded at 4×105 cells/mL in 50 μL growth medium (Ham's F-12 media supplemented with 10% fetal bovine serum, 50,000 units each penicillin and streptomycin, and 500 μg/mL gentamicin) per well in 96-well plates. After 6 to 8 hours, the growth medium is replaced with 50 μL serum-depleted medium (as above, but with 0.1% fetal bovine serum) and cells are incubated overnight. Immediately before compound addition, the medium was replaced with 95 μL serum-depleted medium. Compounds are diluted in 100% DMSO, added to the cells at a final DMSO concentration of 0.25% v/v, and incubated at 37°C for 10 minutes. Cells are stimulated with the appropriate ligand and incubated as above for an additional 8 minutes. The medium is removed and the cells washed once with PBS, then lysed with 50 μL HNTG buffer [20 mmol/L HEPES (pH 7.5), 150 mmol/L NaCl, 2% Triton X-100, 10% glycerol, 5 μmol/L EDTA, 2 mmol/L NaVO4, and 1 EDTA-free complete protease inhibitor tablet per 25 mL] for 5 minutes at room temperature. Lysates are then diluted with 50 μL HG buffer [20 mmol/L HEPES (pH 7.5), 10% glycerol]. The diluted cell lysates are mixed thoroughly, 50 μL of supernatant are transferred to the ELISA capture plate, and incubated at room temperature for 2 hours with agitation. ELISA capture plates are prepared by coating 96-well ReactiBind goat-antirabbit plates with 100 μL/well of 5 μg/mL rabbit anti-human PDGFR-h, anti-PDGFR-a, or anti-VEGFR-2 antibody for 60 to 90 minutes. At the end of the 2-hour incubation the plates are washed (PBS, 0.1% Tween 20) before incubation with anti-phosphotyrosine-horseradish peroxidase antibody (diluted in PBS, 0.05% Tween 20) for 30 minutes at room temperature. The plates are washed again, then incubated with tetramethylbenzidine and evaluated as described above. IC50 values are calculated as percent inhibition of control.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Athymic female mice
  • Formulation: 5% Gelucire
  • Dosages: 3, 10, or 33 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 28 mg/mL warmed (67.06 mM)
Ethanol 4 mg/mL (9.58 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
30% PEG 400+5% propylene glycol+1% Tween 80+ddH2O
For best results, use promptly after mixing.
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 417.5
Formula

C24H27N5O2

CAS No. 343787-29-1
Storage powder
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    I need to formulate CP-673451 for animal studies via oral gavage, any suggestions?

  • Answer:

    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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID