Cat. No.: HY-10321

PD173074

22 Cited Publications

Customer Review

Based on 22 publication(s) in Google Scholar

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.

Purity: 99.86%
CAS No.: 219580-11-7
Formula: C₂₈H₄₁N₇O₃
Molecular Weight:523.67

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

PD173074 Chemical Structure

CAS No.: 219580-11-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (22)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

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)

All VEGFR Isoforms :

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 (K_i) 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.

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.

Chemical Information

CAS No. 219580-11-7
Appearance Solid
Molecular Weight 523.67
Formula C₂₈H₄₁N₇O₃
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

Publications (22)

All In Vivo Efficacy StudyOthersIn Vivo ImagingHistological Imaging/StainingWB

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Journal Impact Factor

Chem Eng J

2025 Sep 15.
Cell Rep Med

Single-cell profiles delineate immune cell remodeling and enhanced tumor-fibroblast interaction of hepatoblastoma after chemotherapy. [Abstract]

2025 Oct 21;6(10):102401. PMID: 41038160

PD173074 purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2025 Oct 21;6(10):102401. [Abstract]

In vivo tumorigenesis assays by vehicle or two TKIs (PD173074, 2 mg/kg, ip; Roblitinib, 50 mg/kg, po) treatment in two subcutaneous PDX models for 30 days.
Cell Death Dis

ONECUT2 facilitates hepatocellular carcinoma metastasis by transcriptionally upregulating FGF2 and ACLY. [Abstract]

2021 Nov 27;12(12):1113. PMID: 34839358

PD173074 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Nov 27;12(12):1113. [Abstract]

Diagram of the administration strategies in vivo. One week after the orthotopic implantation, the nude mice were administered PD173074 (50 mg/kg), ETC-1002 (30 mg/kg) or PD173074 combined with ETC-1002.

PD173074 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Nov 27;12(12):1113. [Abstract]

PD173074 combined with ETC-1002 markedly inhibited ONECUT2-enhanced HCC metastasis. Representative bioluminescent imaging.

PD173074 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Nov 27;12(12):1113. [Abstract]

PD173074 combined with ETC-1002 markedly inhibited ONECUT2-enhanced HCC metastasis. H&E staining of the lungs among four groups of nude mice treated with different administration strategies (n = 10 in each group) for 8 weeks following orthotopic implantation of PLC/PRF/5-ONECUT2 cells.

PD173074 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Nov 27;12(12):1113. [Abstract]

Protein levels of p-AMPKα, AMPKα, p-FGFR1, and FGFR1 were measured in ONECUT2-overexpressing PLC/PRF/5 cells after treatment with PD173074 (5 μM, 12 h), ETC-1002 (100 μM, 12 h) or PD173074 combined with ETC-1002 by western blotting.
EMBO Mol Med

An FGFR3/MYC positive feedback loop provides new opportunities for targeted therapies in bladder cancers. [Abstract]

2018 Apr;10(4). pii: e8163. PMID: 29463565

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.
Br J Pharmacol

A long-acting FGF21 attenuates metabolic dysfunction-associated steatohepatitis-related fibrosis by modulating NR4A1-mediated Ly6C phenotypic switch in macrophages. [Abstract]

2024 Aug;181(16):2923-2946. PMID: 38679486
JCI Insight

FGF-2 signaling in nasopharyngeal carcinoma modulates pericyte-macrophage crosstalk and metastasis. [Abstract]

2022 May 23;7(10):e157874. PMID: 35439170
Atherosclerosis

Inhibition of vascular neointima hyperplasia by FGF21 associated with FGFR1/Syk/NLRP3 inflammasome pathway in diabetic mice. [Abstract]

2019 Oct;289:132-142. PMID: 31513948
Cell Prolif

Flavonoid chrysin activates both TrkB and FGFR1 receptors while upregulates their endogenous ligands such as brain derived neurotrophic factor to promote human neurogenesis. [Abstract]

2025 Jan;58(1):e13732. PMID: 39331585
Int J Mol Sci

Inhibition of Fibroblast Growth Factor Receptor 3 Signaling by Ponatinib Reduces Growth and Cytokine Production of Multiple Myeloma Cells. [Abstract]

2026 Jun 9;27(12):5217. PMID: 42352940
Int J Cancer

FGFR2-RUNX2 activation: An unexplored therapeutic pathway in luminal breast cancer related to tumor progression. [Abstract]

2025 May 15;156(10):2024-2038. PMID: 39731522
J Infect Dis

FGF8 protects against polymicrobial sepsis by enhancing the host's anti-infective immunity. [Abstract]

2024 Nov 18:jiae559. PMID: 39556487
FEBS J

Critical role of the fibroblast growth factor signalling pathway in Ewing's sarcoma octamer-binding transcription factor 4-mediated cell proliferation and tumorigenesis. [Abstract]

2019 Nov;286(22):4443-4472. PMID: 31155838
J Neurosci

Inhibition of FGF Receptor-1 Suppresses Alcohol Consumption: Role of PI3 Kinase Signaling in Dorsomedial Striatum. [Abstract]

2019 Oct 2;39(40):7947-7957. PMID: 31375540
Am J Cancer Res

Long non-coding RNA ANRIL promotes tumorgenesis through regulation of FGFR1 expression by sponging miR-125a-3p in head and neck squamous cell carcinoma. [Abstract]

2018 Nov 1;8(11):2296-2310. PMID: 30555745
Mol Biol Rep

Dapagliflozin promotes browning of white adipose tissue through the FGFR1-LKB1-AMPK signaling pathway. [Abstract]

2024 Apr 21;51(1):562. PMID: 38644407
J Cardiovasc Pharmacol

Inhibition of FGFR Signaling With PD173074 Ameliorates Monocrotaline-induced Pulmonary Arterial Hypertension and Rescues BMPR-II Expression. [Abstract]

2015 Nov;66(5):504-14. PMID: 26535780

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.
bioRxiv

Contribution of S1pr1 -featured astrocyte subpopulation to cisplatin-induced neuropathic pain. [Abstract]

2025 Apr 5:2025.04.03.642851. PMID: 40236155
SSRN

2025 Apr 1.
bioRxiv

2024 November 28.
bioRxiv

Endogenous FGFs drive ERK-dependent cell fate patterning in 2D human gastruloids. [Abstract]

2024 Jul 11:2024.07.08.602611. PMID: 39026750
Patent

US20220305015A1.
Patent

US20180263995A1.

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9096 mL

9.5480 mL

19.0960 mL

5 mM

0.3819 mL

1.9096 mL

3.8192 mL

10 mM

0.1910 mL

0.9548 mL

1.9096 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocol

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.

MedChemExpress (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.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Mohammadi M, et al. Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain. EMBO J. 1998 Oct 15;17(20):5896-904. [Content Brief]

[2]. Skaper SD, et al. The FGFR1 inhibitor PD 173074 selectively and potently antagonizes FGF-2 neurotrophic and neurotropic effects. J Neurochem. 2000 Oct;75(4):1520-7. [Content Brief]

[3]. Bansal R, et al. Specific inhibitor of FGF receptor signaling: FGF-2-mediated effects on proliferation, differentiation, and MAPK activation are inhibited by PD173074 in oligodendrocyte-lineage cells. J Neurosci Res. 2003 Nov 15;74(4):486-93. [Content Brief]

[4]. Trudel S, et al. Inhibition of fibroblast growth factor receptor 3 induces differentiation and apoptosis in t(4;14) myeloma. Blood. 2004 May 1;103(9):3521-8. [Content Brief]

[5]. Mahe M, et al. An FGFR3/MYC positive feedback loop provides new opportunities for targeted therapies in bladder cancers. EMBO Mol Med. 2018 Apr;10(4). pii: e8163. [Content Brief]

[6]. Zheng Y, et al. Inhibition of FGFR Signaling With PD173074 Ameliorates Monocrotaline-induced Pulmonary Arterial Hypertension and Rescues BMPR-II Expression. J Cardiovasc Pharmacol. 2015 Nov;66(5):504-14. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

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PD173074

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) PD173074

All VEGFR Isoforms

Biological Activity

Chemical Information

Publications (22)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PD173074 Related Classifications

Cat. No.: HY-10321