SU 5402
Based on 13 publication(s) in Google Scholar
SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.
For research use only. We do not sell to patients.
- Purity: 99.78%
- CAS No.: 215543-92-3
- Formula: C17H16N2O3
- Molecular Weight:296.32
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) SU 5402
More- J Hazard Mater. 2020 Jul 5;393:122440. [Abstract]
- EMBO J. 2025 Nov 24. [Abstract]
- J Genet Genomics. 2022 Dec;49(12):1101-1113. [Abstract]
- Cells. 2026 Jan 5;15(1):87. [Abstract]
- Int J Mol Sci. 2025 Jul 30;26(15):7361. [Abstract]
- Int J Mol Sci. 2024 Apr 9;25(8):4138. [Abstract]
- iScience. 2019 Sep 27;19:1248-1259. [Abstract]
- Theriogenology. 2019 Jul 1:132:27-35. [Abstract]
- Theriogenology. 2019 Nov:139:90-97. [Abstract]
- bioRxiv. 2024 Feb 2.
- bioRxiv. 2023 Jun 12.
- bioRxiv. 2023 Feb 15.
- bioRxiv. 2023 Feb 8.
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Histological Imaging/Staining
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WB
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IF
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RT-PCR
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Cell Proliferation/Viability Assay
All VEGFR Isoforms
More
Biological Activity
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VEGFR2 20 nM (IC50) |
FGFR1 30 nM (IC50) |
PDGFRβ 510 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HUVEC | IC50 |
>50 μM
Compound: 2
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Evaluated for the inhibition of cell proliferation induced by EGF in HUVEC or NIH3T3 cells
Evaluated for the inhibition of cell proliferation induced by EGF in HUVEC or NIH3T3 cells
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[PMID: 10893303] |
| HUVEC | IC50 |
0.05 μM
Compound: 2
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Evaluated for the inhibition of cell proliferation induced by VEGF in HUVEC or NIH3T3 cells
Evaluated for the inhibition of cell proliferation induced by VEGF in HUVEC or NIH3T3 cells
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[PMID: 10893303] |
| HUVEC | IC50 |
2.8 μM
Compound: 2
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Evaluated for the inhibition of cell proliferation induced by FGF in HUVEC or NIH3T3 cells
Evaluated for the inhibition of cell proliferation induced by FGF in HUVEC or NIH3T3 cells
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[PMID: 10893303] |
| HUVEC | IC50 |
28.4 μM
Compound: 2
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Evaluated for the inhibition of cell proliferation induced by PDGF in HUVEC or NIH3T3 cells
Evaluated for the inhibition of cell proliferation induced by PDGF in HUVEC or NIH3T3 cells
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[PMID: 10893303] |
| NIH3T3 | IC50 |
10 μM
Compound: SU-5402
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Inhibition of acidic FGF-stimulated FGFR1 tyrosine autophosphorylation in mouse NIH/3T3 cells by immunoblotting
Inhibition of acidic FGF-stimulated FGFR1 tyrosine autophosphorylation in mouse NIH/3T3 cells by immunoblotting
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[PMID: 9139660] |
SU 5402 is cocrystallized with the catalytic domain of FGF-R1 (flg-1) and is found to inhibit tyrosine phosphorylation of VEGF-R2 (Flk-1/KDR) and PDGF-R in NIH 3T3 cells with IC50 values of 0.4 and 60.9 μM, respectively[1]. In order to investigate whether phosphorylation of PKM2 and LDHA is mediated in FGFR1-specific manner, FTC-133 are treated with receptor tyrosine kinase inhibitors Dovitinib and SU 5402 (SU-5402). Dovitinib treatment results in significant decrease of phosphorylation status at a concentration of 100 nM after four hours of incubation for both PKM2 and LDHA. No significant changes are seen when administered at concentrations of 1 nM and 10 nM. SU 5402 administration leads to a sigificant decrease of PKM2 and LDHA phosphorylation at a concentration of 20 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 215543-92-3
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Appearance Solid
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Molecular Weight 296.32
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Formula C17H16N2O3
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Color Light brown to orange
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SMILES
O=C(CCC1=C(NC=C1C)/C=C2C(NC3=C\2C=CC=C3)=O)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (13)
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Journal Impact Factor
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Most Recent
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J Hazard Mater
Non-cytotoxic silver nanoparticle levels perturb human embryonic stem cell-dependent specification of the cranial placode in part via FGF signaling. [Abstract]2020 Jul 5;393:122440. PMID: 32151936
SU 5402 purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2020 Jul 5;393:122440. [Abstract]
Shown are the qRT-PCR analyses for the expression of FGF related genes, after treatment with SU 5402 (30 nM) and 0.1 μg/mL AgNPs or AgNO3, for 12 days during the differentiation.
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EMBO J
BMP4 initiates and patterns ventral-caudal structures in zebrafish and human pluripotent stem cell aggregates. [Abstract]2025 Nov 24. PMID: 41286028
SU 5402 purchased from MedChemExpress. Usage Cited in: EMBO J. 2025 Nov 24. [Abstract]
WISH of tbxta, cdx4 in Bmp4 explants treated with Nodal inhibitor (SB505124, 50 μM), Wnt inhibitor (IWP-L6, 25 μM) or SU 5402 (25 μM) at 6 hpf, with injection sites oriented to the right. Representative images of treated or untreated Bmp4 explants at 24 hpf are displayed.
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J Genet Genomics
Cdx1b protects intestinal cell fate by repressing signaling networks for liver specification. [Abstract]2022 Dec;49(12):1101-1113. PMID: 36460297 -
Cells
Caffeine Mitigates Adenosine-Mediated Angiogenic Properties of Choroidal Endothelial Cells Through Antagonism of A1 Adenosine Receptor and PI3K-AKT Axis. [Abstract]2026 Jan 5;15(1):87. PMID: 41511370 -
Int J Mol Sci
Direct and Indirect Downstream Pathways That Regulate Repulsive Guidance Effects of FGF3 on Developing Thalamocortical Axons. [Abstract]2025 Jul 30;26(15):7361. PMID: 40806490
SU 5402 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Jul 30;26(15):7361. [Abstract]
The FGFR inhibitor SU 5402 (20 μM) reduced the expression of the repellent factor Slit1.
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Int J Mol Sci
Small Molecules Promote the Rapid Generation of Dental Epithelial Cells from Human-Induced Pluripotent Stem Cells. [Abstract]2024 Apr 9;25(8):4138. PMID: 38673725
SU 5402 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Apr 9;25(8):4138. [Abstract]
SU 5402 (10 μM; 4 d). Brightfield indicated the cell morphology and immunostaining of markers for NNE, stemness and PPE on day 4 of differentiation. The change in cell morphology and immunostaining of the NNE marker TFAP2A (red), the stemness marker OCT4 (red), and the PPE marker SIX1 (green) were also indicated. Arrows indicated SIX1+ cells.
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iScience
2019 Sep 27;19:1248-1259. PMID: 31353167 -
Theriogenology
Reciprocal stimulating effects of bFGF and FSH on chicken primordial follicle activation through AKT and ERK pathway. [Abstract]2019 Jul 1:132:27-35. PMID: 30986612 -
Theriogenology
Basic fibroblast growth factor promotes prehierarchical follicle growth and yolk deposition in the chicken. [Abstract]2019 Nov:139:90-97. PMID: 31400551
SU 5402 purchased from MedChemExpress. Usage Cited in: Theriogenology. 2019 Nov:139:90-97. [Abstract]
Effect of bFGF and SU5402 on BrdU incorporation in proliferating cells and TUNEL labeling of the apoptotic cells. Red fluorescence: BrdU-labelled cells, mainly distributed in the follicular theca externa. Green fluorescence: TUNEL -labelled cells. Blue fluorescence: DAPI staining. DeE: The percentage of BrdU-positive cells and TUNEL-positive cells. SU 5402 blocks the ability of bFGF to significantly increase the ratio of BrdU-labelled cells. The opposite situation was observed in the results of TUNEL assay.
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Solvent & Solubility
DMSO : ≥ 30 mg/mL (101.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.44 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
8505C and FTC133 cells are grown in DMEM/F12 suppplemented with 10% FCS and 1% PenStrep and incubated at 37°C, 5% CO2. For B-CPAP RPMI 1640 medium is used. FGFR1 inhibition experiments are performed on FTC133 cells by employment of Receptor Tyrosine Kinase Inhibitors TKI-258 (Dovitinib) and SU 5402 (20μM). Inhibition is conducted over 4 h with the indicated inhibitor concentrations. Control cells receive corresponding concentrations of DMSO[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
Male ΔF508 mice (CFTRtm1Eur on a 129/FVB background) and their wild-type littermates of 9-12 weeks are intraperitoneally injected with DMSO or SU 5402 (dissolved in DMSO at the concentration of 6 mg/mL) at 25 mg/kg body weight, every day for 1 week. The mice are weighed daily and the dosages adjusted accordingly. The mice are then anesthetized by inhaling isoflurane until the end of the procedure. Cholinergic antagonist, Atropine (1 mM, 50 μL) is subcutaneously injected into the right cheek to block potential cholinergic stimulation of the salivary gland. A small strip of filter paper is placed against the injected cheek, for 4 min. Isoprenaline (10 mM, 37.5 μL) is subsequently injected in the same spot to stimulate an adrenergic secretion of saliva (time 0). Filter strips (pre-weighed in an Eppendorf tube) are replaced every 5 min, over a period of 30 min. All six filter strips are weighed at the end of the collection and the results are normalized relative to mg/g body weight.
Rats[4]
To assess the potential effects of the FGFR1 inhibitor SU 5402 on established PH, adult male Wistar rats (200-250 g) are given MCT (60 mg/kg s.c.), left untreated for 21 days, then randomly divided into 2 groups (10 animals in each group), of which one is treated with SU 5402 (25 mg/kg/day) and the other given the vehicle, from day 21 to day 42. All treatments are given once a day by s.c. injection.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (284 KB)
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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)
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Handling Instructions (2659 KB)
References
[1]. Sun L, et al. Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases. J Med Chem. 1999 Dec 16;42(25):5120-30. [Content Brief]
[2]. Kachel P, et al. Phosphorylation of pyruvate kinase M2 and lactate dehydrogenase A by fibroblast growth factor receptor 1 in benign and malignant thyroid tissue. BMC Cancer. 2015 Mar 18;15:140. [Content Brief]
[3]. Trzcińska-Daneluti AM, et al. RNA Interference Screen to Identify Kinases That Suppress Rescue of ΔF508-CFTR. Mol Cell Proteomics. 2015 Jun;14(6):1569-83. [Content Brief]
[4]. Izikki M, et al. Endothelial-derived FGF2 contributes to the progression of pulmonary hypertension in humans and rodents. J Clin Invest. 2009 Mar;119(3):512-23. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3747 mL | 16.8736 mL | 33.7473 mL | 84.3682 mL |
| 5 mM | 0.6749 mL | 3.3747 mL | 6.7495 mL | 16.8736 mL | |
| 10 mM | 0.3375 mL | 1.6874 mL | 3.3747 mL | 8.4368 mL | |
| 15 mM | 0.2250 mL | 1.1249 mL | 2.2498 mL | 5.6245 mL | |
| 20 mM | 0.1687 mL | 0.8437 mL | 1.6874 mL | 4.2184 mL | |
| 25 mM | 0.1350 mL | 0.6749 mL | 1.3499 mL | 3.3747 mL | |
| 30 mM | 0.1125 mL | 0.5625 mL | 1.1249 mL | 2.8123 mL | |
| 40 mM | 0.0844 mL | 0.4218 mL | 0.8437 mL | 2.1092 mL | |
| 50 mM | 0.0675 mL | 0.3375 mL | 0.6749 mL | 1.6874 mL | |
| 60 mM | 0.0562 mL | 0.2812 mL | 0.5625 mL | 1.4061 mL | |
| 80 mM | 0.0422 mL | 0.2109 mL | 0.4218 mL | 1.0546 mL | |
| 100 mM | 0.0337 mL | 0.1687 mL | 0.3375 mL | 0.8437 mL |