製品番号: HY-10407

SU 5402

13 Cited Publications

カスタマーレビュー

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.

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純度: 99.78%
CAS 番号: 215543-92-3
分子式: C₁₇H₁₆N₂O₃
分子量:296.32

保管条件:

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

SU 5402 構造式

CAS 番号: 215543-92-3

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価格（税別）

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数量

Amount: USD 0.00

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (13)
溶剤 & 溶解度
- 体外
- 体内
プロトコル
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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.

IC₅₀ & Target^[1]

VEGFR2

20 nM (IC₅₀)

FGFR1

30 nM (IC₅₀)

PDGFRβ

510 nM (IC₅₀)

VEGFR アイソフォーム固有の製品をすべて表示 :

PDGFR アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
HUVEC	IC₅₀	>50 μM Compound: 2	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	[PMID: 10893303]
HUVEC	IC₅₀	0.05 μM Compound: 2	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	[PMID: 10893303]
HUVEC	IC₅₀	2.8 μM Compound: 2	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	[PMID: 10893303]
HUVEC	IC₅₀	28.4 μM Compound: 2	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	[PMID: 10893303]
NIH3T3	IC₅₀	10 μM Compound: SU-5402	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	[PMID: 9139660]

体外実験

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.

体内実験

Inhibition of FGFR1 with SU 5402 (SU5402) administered to ΔF508-CFTR homozygous mice results in partial ΔF508-CFTR rescue, as shown by an increase in saliva secretion, a surrogate "sweat test" assay in mice. As salivary secretion is often sex dependent, only male mice are chosen for these experiments. Our results indicate that treatment of the ΔF508-CFTR mice with SU 5402 restores the saliva secretion level to ~10% of that observed for the wild-type CFTR mice, which suggests that SU 5402 can have therapeutic benefits to Cystic Fibrosis (CF)^[3]. The selective FGFR1 inhibitor SU 5402 (SU5402) prevents and/or reverses PH induced by MCT (monocrotaline) in rats. In rats treated with SU 5402 on days 21 to 42 after the MCT injection, evaluations on day 42 show marked decreases in pulmonary artery pressure (PAP), RV/(LV+S), and distal artery muscularization compare with rats treated with the vehicle (saline)^[4].

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

化学情報

CAS 番号 215543-92-3
性状 Solid
分子量 296.32
分子式 C₁₇H₁₆N₂O₃
Color Light brown to orange
SMILES

O=C(CCC1=C(NC=C1C)/C=C2C(NC3=C\2C=CC=C3)=O)O
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

Publications (13)

All RT-PCRHistological Imaging/StainingWBIFCell Proliferation/Viability Assay

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Journal Impact Factor

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.
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.
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.
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.
iScience

Evolution and Developmental Diversity of Skin Spines in Pufferfishes. [Abstract]

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.
bioRxiv

2024 Feb 2.
bioRxiv

2023 Jun 12.
bioRxiv

2023 Feb 15.
bioRxiv

2023 Feb 8.

溶剤 & 溶解度

体外:

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.

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

3.3747 mL

16.8736 mL

33.7473 mL

5 mM

0.6749 mL

3.3747 mL

6.7495 mL

10 mM

0.3375 mL

1.6874 mL

3.3747 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, 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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

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 (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.

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

プロトコル

Cell Assay^[2]

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.

Animal Administration^[3]^[4]

Mice^[3]
Male ΔF508 mice (CFTR^tm1Eur 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.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
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取扱説明書 (2659 KB)

参考文献

[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]

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, 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

Keywords

SU 5402

13 Cited Publications

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SU 5402

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Differentiation Inducing Compound Library

Reprogramming 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

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

MedChemExpress（MCE）の使用を引用している文献 SU 5402

VEGFR アイソフォーム固有の製品をすべて表示

PDGFR アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (13)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

SU 5402 関連分類

HY-10407 関連分類