2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FGFR VEGFR Apoptosis
  4. PD173074

PD173074 is a potent FGFR1 inhibitor with an IC50 of 25 nM and also inhibits VEGFR2 with an IC50 of 100-200 nM, showing 1000-fold selectivity for FGFR1 over PDGFR and c-Src.

For research use only. We do not sell to patients.

PD173074 Chemical Structure

PD173074 Chemical Structure

CAS No. : 219580-11-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 73 In-stock
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50 mg USD 185 In-stock
100 mg USD 290 In-stock
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Customer Review

Based on 16 publication(s) in Google Scholar

PD173074 Related Antibodies

Top Publications Citing Use of Products

    PD173074 purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2018 Apr;10(4). pii: e8163.  [Abstract]

    Western blot analysis of MYC and FGFR3 expression in lysates from MGH-U3 and RT112 cells treated with (+)-JQ1 (1 or 4 μM) for 48 h. Anti-actin antibody is used as a loading control. Pan-FGFR inhibitor, PD173074 (50 nM and 1 μM), and inactive enantiomer (-)-JQ1 (4 μM) are used as controls.

    PD173074 purchased from MedChemExpress. Usage Cited in: J Cardiovasc Pharmacol. 2015 Nov;66(5):504-14.  [Abstract]

    The effects of PD173074 on expression and activation of Akt, Erk1/2, PCNA, and caspase-3 representative immunoblots of Akt, Erk1/2, PCNA, a-SMA, cleaved caspase-3, Bcl-2, and Bax. GAPDH is a loading control.

    View All FGFR Isoform Specific Products:

    View All Isoforms
    FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

    View All VEGFR Isoform Specific Products:

    View All Isoforms
    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PD173074 is a potent FGFR1 inhibitor with an IC50 of 25 nM and also inhibits VEGFR2 with an IC50 of 100-200 nM, showing 1000-fold selectivity for FGFR1 over PDGFR and c-Src.

    IC50 & Target[1]

    FGFR1

    25 nM (IC50)

    VEGFR2

    100 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    NCI-H520 IC50
    281 nM
    Compound: PD173074
    Antiproliferative activity against human FGFR1-amplified NCI-H520 cells after 7 days by SRB assay
    Antiproliferative activity against human FGFR1-amplified NCI-H520 cells after 7 days by SRB assay
    		[PMID: 28521156]
    RT-112 GI50
    0.015 μM
    Compound: PD173074
    Antiproliferative activity against human RT112 cells after 72 hrs by MTT assay
    Antiproliferative activity against human RT112 cells after 72 hrs by MTT assay
    		[PMID: 27599742]
    SUM185PE IC50
    20 nM
    Compound: 58; PD173074
    Anticancer activity against human SUM185PE cells assessed as cell growth inhibition incubated for 6 days by CellTiter96 analysis
    Anticancer activity against human SUM185PE cells assessed as cell growth inhibition incubated for 6 days by CellTiter96 analysis
    		[PMID: 33650861]
    SW780 IC50
    84.3 nM
    Compound: PD173074
    Antiproliferative activity against human FGFR3-amplified SW780 cells after 5 days by SRB assay
    Antiproliferative activity against human FGFR3-amplified SW780 cells after 5 days by SRB assay
    		[PMID: 28521156]
    In Vitro

    PD 173074 inhibits autophosphorylation of FGFR1 in a dose-dependent manner with an IC50 in the range 1-5 nM. PD 173074 is an ATP-competitive inhibitor of FGFR1 with an inhibitory constant (Ki) of 40 nM[1]. PD 173074 and SU 5402 produce concentration-dependent reductions in FGF-2 enhancement of granule neuron survival, with IC50 values of 8 nM and 9 μM, respectively. PD 173074 does not inhibit neurotrophic and neuritogenic actions of FGF-2 signalling molecules in cerebellar granule neurons. PD 173074 and SU 5402 concentration-dependently inhibits the neurite growth response, when tested on FGF-2-treated granule neurons growing on polylysine/laminin, with IC50s of 22 nM and 25 μM, respectively[2]. PD173074 effectively antagonizes the effect of FGF-2 on proliferation and differentiation of OL progenitors in culture. Mitogen-activated protein kinase (MAPK) activation, a downstream event after activation of either FGFR or PDGFR, is also blocked by PD173074 in OL progenitors stimulated with FGF-2 but not PDGF[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    PD173074 Related Antibodies
    In Vivo

    PD 173074 (1 mg/kg, i.p.) exhibits dose-dependent inhibition of FGF-induced neovascularization and angiogenesis in mice[1]. D173074 (25 mg/kg, p.o.) significantly inhibits tumor growth in mice[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    523.67

    Formula

    C28H41N7O3
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    O=C(NC1=NC2=NC(NCCCCN(CC)CC)=NC=C2C=C1C3=CC(OC)=CC(OC)=C3)NC(C)(C)C
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (190.96 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9096 mL 9.5480 mL 19.0960 mL
    5 mM 0.3819 mL 1.9096 mL 3.8192 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.77 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.77 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.70%

    SDS (393 KB)

    COA (247 KB) LCMS (266 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    An NIH 3T3 cell line overexpressing VEGFR2 (Flk-1) has been described previously. This cell line also expresses FGFR1 endogenously. Cells (1×106) in DMEM supplemented with 10% calf serum are seeded in 10 cm2 dishes and allowed to grow for 48 h. The medium is then removed and the cells are made quiescent in starvation medium (DMEM with 0.1% calf serum). After 18 h, the cells are incubated for 5 min with various concentrations of PD 173074 prepared in starvation medium. The cells are then stimulated with growth factor [VEGF (100 ng/mL) or aFGF (100 ng/mL) and heparin (10 µg/mL)] for 5 min at 37°C. The cells are washed with ice-cold PBS and lysed in 1 mL of lysis buffer (25 mM HEPES pH 7.5, 150 mM NaCl, 1% Triton X-100, 10% glycerol, 1 mM EGTA, 1.5 mM MgCl2, 1 mM PMSF, 10 µg/mL aprotonin, 10 µg/mL leupeptin) containing phosphatase inhibitor (0.2 mM Na3VO4). For inhibition studies of FGFR1, cell lysates are immunoprecipitated with antibodies to FGFR1, and then analyzed by SDS-PAGE and immunoblotting with antibodies to phosphotyrosine. For inhibition studies of VEGFR2, cell lysates (20 µL) are analyzed directly by SDS-PAGE and immunoblotted with antibodies to phosphotyrosine.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [4]

    Six-week-old athymic nude mice are inoculated subcutaneously with 3×105 NIH 3T3 cells expressing Y373C FGFR3 and Ras V12. Intraperitoneal injections of either 20 mg/kg PD173074 or 0.05 mol/Llactic acid buffer are initiated on the day of tumor injection and continued for 9 days. Ten mice for each experiment are included.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9096 mL 9.5480 mL 19.0960 mL 47.7400 mL
    5 mM 0.3819 mL 1.9096 mL 3.8192 mL 9.5480 mL
    10 mM 0.1910 mL 0.9548 mL 1.9096 mL 4.7740 mL
    15 mM 0.1273 mL 0.6365 mL 1.2731 mL 3.1827 mL
    20 mM 0.0955 mL 0.4774 mL 0.9548 mL 2.3870 mL
    25 mM 0.0764 mL 0.3819 mL 0.7638 mL 1.9096 mL
    30 mM 0.0637 mL 0.3183 mL 0.6365 mL 1.5913 mL
    40 mM 0.0477 mL 0.2387 mL 0.4774 mL 1.1935 mL
    50 mM 0.0382 mL 0.1910 mL 0.3819 mL 0.9548 mL
    60 mM 0.0318 mL 0.1591 mL 0.3183 mL 0.7957 mL
    80 mM 0.0239 mL 0.1193 mL 0.2387 mL 0.5967 mL
    100 mM 0.0191 mL 0.0955 mL 0.1910 mL 0.4774 mL
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    PD173074 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    PD173074219580-11-7PD 173074PD-173074FGFRVEGFRApoptosisFibroblast growth factor receptorVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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