1. Protein Tyrosine Kinase/RTK
  2. PDGFR

CP-673451 

Cat. No.: HY-12050 Purity: 99.65%
Data Sheet SDS Handling Instructions

CP-673451 is a potent selective inhibitor of platelet-derived growth factor receptor (PDGFR), and inhibits PDGFR-α and PDGFR-β kinase with IC50s of 10 and 1 nM, respectively.

For research use only. We do not sell to patients.
CP-673451 Chemical Structure

CP-673451 Chemical Structure

CAS No. : 343787-29-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $150 In-stock
5 mg $136 In-stock
10 mg $256 In-stock
50 mg $776 In-stock
100 mg $1050 In-stock
200 mg   Get quote  
500 mg   Get quote  

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    CP-673451 purchased from MCE. Usage Cited in: FASEB J. 2016 Nov;30(11):3733-3744.

    Autocrine activation of receptor tyrosine kinases (RTKs) is required for induction of GLUT1 by TGF-b. Quantitative RT-PCR analysis of 10 ng/mL TGF-b1–stimulated GLUT1 expression (12 h post treatment) in AKR-2B cells in the presence of the PDGFR specific inhibitor, CP673451 (2 μM).
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    CP-673451 is a potent selective inhibitor of platelet-derived growth factor receptor (PDGFR), and inhibits PDGFR-α and PDGFR-β kinase with IC50s of 10 and 1 nM, respectively.

    IC50 & Target

    IC50: 10 nM (PDGFR-α), 1 nM (PDGFR-β)[4]

    In Vitro

    CP-673451 efficiently suppresses the PDGFR downstream signaling pathway. It inhibits phosphorylation of Akt, GSK-3β, p70S6, and S6 in A549 cells in a concentration-dependent manner. CP-673451 (0.0625-4 μM) significantly reduces the viability of NSCLC cell lines A549 and H1299 in a time- and concentration-dependent manner, with IC50s of 0.49 and 0.61 μM, respectively. CP-673451 (1, 4 μM) induces apoptosis in non-small-cell lung cancer cells. CP-673451 (25, 100, or 400 nM) is effective at inhibiting migration and invasion of NSCLC cells by suppression of lamellipodia formation[1]. CP-673451 and crenolanib show selective lethality toward cells with CA. U2OS cells treated with 1 to 4 μM CP-673451 or crenolanib show a ruffled cell surface as a sign for alterations of the cortical actin cytoskeleton. CP-673451 attenuates PDGF-BB-induced signaling, and significantly enhances the phosphorylation of PDGFR-β downstream effectors, Akt and MEK[2]. CP-673,451 (0.5 μM) regulates cell proliferation through mechanisms involving reduced phosphorylation of GSK-3α and GSK-3β. CP-673,451 impairs rhabdosphere-forming capacity in both RD and RUCH2 cultures[3]. CP-673,451 inhibits PDGFR-β in PAE-β cells with an IC50 value of 6.4 nM. Besides, CP-673,451 incubation in H526 and PAE-β cells results in an IC50 value of 1.1 μM against c-kit[4].

    In Vivo

    CP-673451 (20 mg/kg) leads to a medium suppression of tumor growth, while high-dose CP-673451 (40 mg/kg) strongly inhibits tumor growth in mice without significant weitht loss[1]. CP-673,451 (10, 33, and 100 mg/kg, p.o., b.i.d) inhibits the growth of Colo205 tumor in a dose-dependent manner, and similar tumor growth inhibition experiments completes on LS174T, H460, and U87MG xenografts, with no signs of morbidity or weight loss[4].

    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 2.3952 mL 11.9760 mL 23.9521 mL
    5 mM 0.4790 mL 2.3952 mL 4.7904 mL
    10 mM 0.2395 mL 1.1976 mL 2.3952 mL
    Cell Assay
    [3]

    CP-673451 is dissolved in DMSO and diluted in serum-reduced medium (1.5 % FBS).

    Cell proliferation/viability is analyzed using the CyQuant proliferation assay. Pre-starved cells are treated every 24 hours with vehicle (dimethyl sulfoxide) or 0.5 μM CP-673,451 diluted in serum-reduced medium (1.5 % FBS) for 96 hours. The amount of nucleic acid present in lysed cells is normalized to the amount when treatment is initiated. Cell proliferation/viability in response to 300 ng/mL PDGF-CC is likewise analyzed, but cells are then kept in serum-free medium and treated twice during a 48-hour period. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    CP-673451 is formulated in 10% 1-methyl-2-pyrrolidinone and 90% polyethylene glycol 300.

    A subcutaneous A549 xenograft model in nude mice is used to evaluate the anticancer activity of CP-673451. Briefly, A549 cells are injected into the axillary regions of mice (2×106 cells/mouse). When the tumor volumes reach 70 mm3, the mice are randomly assigned to a control group and two CP-673451 groups (n=6 per group): low-dose (20 mg/kg) and high dose (40 mg/kg) groups (vehicle 10% 1-methyl-2-pyrrolidinone and 90% polyethylene glycol 300). These animals are administered intraperitoneally with CP-673451 (20 or 40 mg/kg/day) or with vehicle. During the treatment period, the implanted tumors are measured by caliper once a day in a blind fashion. The animal body weights are also measured at the same time. The tumor volume is calculated as follows: (width × width × length)/2. After treatment, the mice are killed, and the tumors are harvested and analyzed. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    417.5

    Formula

    C₂₄H₂₇N₅O₂

    CAS No.

    343787-29-1

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.65%

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    CP-673451
    Cat. No.:
    HY-12050
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