PD 173074
PD 173074 (CAS 219580-11-7) is a potent and selective small molecule inhibitor belonging to the class of tyrosine kinase inhibitors, functioning as a selective antagonist of fibroblast growth factor receptor (FGFR) in cellular systems and exhibiting high selectivity against other related kinases. Additionally, it demonstrates inhibition of related signaling pathways downstream of FGFR activation.
In in vitro enzymatic assays, PD 173074 inhibits FGFR activity with an IC50 value of 25 nM, tested against purified FGFR proteins. It is also capable of suppressing other tyrosine kinase activities with measured IC50 values in the range of 100–200 nM, tested in comparison to kinases such as VEGFR and others. In contrast, its inhibitory effect against kinases such as c-Src is more than 1000-fold less potent than against FGFR, highlighting its high degree of specificity. Further studies indicate that PD 173074 can block FGFR-driven signaling cascades and reduce cell proliferation in FGFR-dependent cell lines. It can also inhibit downstream phosphorylation events associated with growth factor signaling, contributing to its overall antagonist activity.
In pharmaceutical and biomedical research, PD 173074 is widely used for mechanistic studies of FGFR signaling, target validation, and as a research tool in the development or screening of FGFR-targeted therapeutics.
- 1. Soher Nagi Jayash, Thomas Duff, et al. "Osteoblasts sense extracellular levels of phosphate to control the local expression of phosphatases for matrix mineralisation." Volume 26, September 2025, 101863
- 2. Cheukyau Luk, Katherine I. Bridge, et al. "Paracrine role of endothelial IGF-1 receptor in depot-specific adipose tissue adaptation in male mice." Nat Commun. 2025 Jan 2;16(1):170. PMID: 39747815
- 3. Abeer Alghamdi, Hussah Alobaid, et al."Inhibitory effect of PD173074 drug on DMBA-induced mammary carcinoma in female Swiss albino mice." January 2025 Tropical Journal of Pharmaceutical Research 23(12):1983-1989
- 4. Day EK, Sosale NG, et al. "Glioblastoma Cell Resistance to EGFR and MET Inhibition Can Be Overcome via Blockade of FGFR-SPRY2 Bypass Signaling." Cell Rep. 2020;30(10):3383-3396.e7. PMID:32160544
- 5. Chen P, Zhang H, et al. "Basic Fibroblast Growth Factor Reduces Permeability and Apoptosis of Human Brain Microvascular Endothelial Cells in Response to Oxygen and Glucose Deprivation Followed by Reoxygenation via the Fibroblast Growth Factor Receptor 1 (FGFR1)/ERK Pathway." Med Sci Monit. 2019 Sep 25;25:7191-7201. PMID:31551405
| Physical Appearance | A solid |
| Storage | Store at 4°C |
| M.Wt | 523.67 |
| Cas No. | 219580-11-7 |
| Formula | C28H41N7O3 |
| Synonyms | PD 173074,PD-173074 |
| Solubility | ≥26.18 mg/mL in DMSO; insoluble in H2O; ≥108.4 mg/mL in EtOH with ultrasonic |
| Chemical Name | 1-tert-butyl-3-[2-[4-(diethylamino)butylamino]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]urea |
| SDF | Download SDF |
| Canonical SMILES | CCN(CC)CCCCNC1=NC2=NC(=C(C=C2C=N1)C3=CC(=CC(=C3)OC)OC)NC(=O)NC(C)(C)C |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Kinase experiment [1]: | |
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In vitro kinase inhibition assays |
Assays using the full-length FGFR-1 kinase were performed in a total volume of 100 μL containing 25 mM HEPES buffer (pH 7.4), 150 mM NaCl, 10 mM MnCl2, 0.2 mM sodium orthovanadate, 750 μg/mL concentration of a random copolymer of glutamic acid and tyrosine (4:1), various concentrations of PD173074 and 60 to 75 ng of enzyme. The reaction was initiated by the addition of [γ-32P]ATP (5 μM ATP containing 0.4 μCi of [γ-32P]ATP per incubation), and samples were incubated at 25 °C for 10 mins. The reaction was terminated by the addition of 30% trichloroacetic acid and the precipitation of material onto glass-fiber filter mats. Filters were washed three times with 15% trichloroacetic acid, and the incorporation of [32P] into the glutamate tyrosine polymer substrate was determined by counting the radioactivity retained on the filters in a Wallac 1250 betaplate reader. |
| Cell experiment [1]: | |
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Cell lines |
NIH 3T3 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months. |
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Reaction Conditions |
0 ~ 1000 nM; 5 mins |
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Applications |
PD 173074 dose-dependently inhibited autophosphorylation of FGFR1, with an IC50 value in the range of 1 ~ 5 nM. In addition, PD 173074 inhibited autophosphorylation of VEGFR2 with an IC50 value of 100 ~ 200 nM. |
| Animal experiment [1]: | |
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Animal models |
Swiss Webster mice with induced corneal angiogenesis |
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Dosage form |
1 or 2 mg/kg/day; i.p. |
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Applications |
At the dose of 1 or 2 mg/kg, PD 173074 significantly inhibited angiogenesis induced by either FGF or VEGF in a dose-dependent manner. Besides, it showed no apparent toxicity. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Mohammadi M, Froum S, Hamby JM, Schroeder MC, Panek RL, Lu GH, Eliseenkova AV, Green D, Schlessinger J, Hubbard SR. Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain. EMBO J. 1998 Oct 15;17(20):5896-904. |
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| Description | PD173074 is a potent inhibitor of FGFR1 with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM, ~1000-fold selective for FGFR1 than PDGFR and c-Src. | |||||
| Targets | FGFR1 | VEGFR2 | ||||
| IC50 | ~25 nM | 100-200 nM | ||||
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