SU5402

Catalog No.S7667 Batch:S766701

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Technical Data

Formula

C17H16N2O3
Molecular Weight 296.32 CAS No. 215543-92-3
Solubility (25°C)* In vitro DMSO 59 mg/mL (199.1 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.
Targets
VEGFR2 [1]
(Cell-free assay)		 FGFR1 [1]
(Cell-free assay)		 PDGFRβ [1]
(Cell-free assay)
20 nM 30 nM 510 nM
In vitro SU5402 inhibits VEGF-, FGF-, PDGF- dependent cell proliferation with IC50 of 0.05 μM, 2.80μM, 28.4 μM, respectively. [1] In HUVECs, SU5416 selectively inhibits VEGF-driven mitogenesis in a dose-dependent manner with IC50 of 0.04 μM. [2] In nasopharyngeal epithelial cells, SU5402 attenuates LMP1-mediated aerobic glycolysis, cellular transformation, cell migration, and invasion. [3] In mouse C3H10T1/2 cells, SU 5402 diminishes the effect of FGF23 on cell differentiation. [4]
In vivo In mice, SU5416 (25 mg/kg, i.p.) inhibits subcutaneous growth of a panel of tumor cell lines by inhibiting the angiogenic process associated with tumor growth. [2]

Protocol (from reference)

Kinase Assay:[1]
  • FGF-R1 and Flk-1/KDR kinase assays.

    The catalytic portion of FGF-R1 and Flk-1/KDR are expressed as GST fusion proteins following infection of Spodoptera frugiperda (sf9) cells with engineered baculoviruses. GST-FGFR1 and GST-Flk1 are purified to homogeneity from infected sf9 cell lysates by glutathione sepharose chromatography. The assays are performed in 96-well microtiter plates that had been coated overnight with 2.0 μg of a polyGlu-Tyr peptide (4:1) in 0.1 mL of PBS per well. The purified kinases are diluted in kinase assay buffer (100 mM Hepes pH 7.5, 100 mM NaCl, and 0.1 mM sodium orthovanadate) and added to all test wells at 5 ng of GST fusion protein per 0.05 mL volume buffer. Test compounds are diluted in 4% DMSO and added to test wells (0.025 mL/well). The kinase reaction is initiated by the addition of 0.025 mL of 40 μM ATP/40 mM MnCl2, and plates are shaken for 10 min before stopping the reactions with the addition of 0.025 mL of 0.5 M EDTA. The final ATP concentration was 10 μM, which is twice the experimentally determined Km value for ATP. Negative control wells receive MnCl2 alone without ATP. The plates are washed three times with 10 mM Tris pH 7.4, 150 mM NaCl, and 0.05% Tween-20 (TBST). Rabbit polyclonal anti-phosphotyrosine antiserum is added to the wells at a 1:10000 dilution in TBST for 1 h. The plates are then washed three times with TBST. Goat anti-rabbit antiserum conjugated with horseradish peroxidase was then added to all wells for 1 h. The plates are washed three times with TBST, and the peroxidase reaction is detected with the addition of 2,2‘-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS). The color readout of the assay is allowed to develop for 20−30 min and read on a Dynatech MR5000 ELISA plate reader using a 410 nM test filter.
Cell Assay:[2]
  • Cell lines

    SF767T, SF763, EPH4-VEGF, C6, A375, A431, LNCAP, Calu-6, 3T3Her2 and 488G2M2 cells

  • Concentrations

    ~50 μM

  • Incubation Time

    96 hours

  • Method

    Tumor cell lines used in the in vitro growth are cultured in media at 37°C in 5–10% CO2. SU5416 is serially diluted in media containing DMSO (<0.5%) and added to cultures of tumor cells 1 day after the initiation of culture. Cell growth is measured after 96 h using the sulforhodamine B method. IC50s are calculated by curve fitting using four-parameter analysis.
Animal Study:[2]
  • Animal Models

    Mice bearing SF767T, SF763, EPH4-VEGF, C6, A375, A431, LNCAP, Calu-6, 3T3Her2 or 488G2M2 tumors

  • Dosages

    25 mg/kg/d

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Oncogene, 2017, 36(6):766-776]

Data from [Data independently produced by , , Angiogenesis, 2017, 20(4):629-640]

Selleck's SU5402 has been cited by 17 publications

Host-to-graft propagation of inoculated α-synuclein into transplanted human induced pluripotent stem cell-derived midbrain dopaminergic neurons [ Regen Ther, 2024, 25:229-237] PubMed: 38283940
Oxidative stress induces lysosomal membrane permeabilization and ceramide accumulation in retinal pigment epithelial cells [ Dis Model Mech, 2023, 16(7)dmm050066] PubMed: 37401371
Generating Neural Retina from Human Pluripotent Stem Cells [ J Vis Exp, 2023, (202).] PubMed: 38189566
Microglia-derived PDGFB promotes neuronal potassium currents to suppress basal sympathetic tonicity and limit hypertension [ Immunity, 2022, S1074-7613(22)00291-6] PubMed: 35863346
Generation of GLA-knockout human embryonic stem cell lines to model peripheral neuropathy in Fabry disease [ Mol Genet Metab Rep, 2022, 33:100914] PubMed: 36092250
Control of osteoblast regeneration by a train of Erk activity waves [ Nature, 2021, 10.1038/s41586-020-03085-8] PubMed: 33408418
Cohesin-protein Shugoshin-1 controls cardiac automaticity via HCN4 pacemaker channel [ Nat Commun, 2021, 12(1):2551] PubMed: 33953173
NOCICEPTRA: Gene and microRNA Signatures and Their Trajectories Characterizing Human iPSC-Derived Nociceptor Maturation [ Adv Sci (Weinh), 2021, 8(21):e2102354] PubMed: 34486248
The cytokine FAM3B/PANDER is an FGFR ligand that promotes posterior development in Xenopus [ Proc Natl Acad Sci U S A, 2021, 118(20)e2100342118] PubMed: 33975953
Role of HRTPT in kidney proximal epithelial cell regeneration: Integrative differential expression and pathway analyses using microarray and scRNA-seq [ J Cell Mol Med, 2021, 10.1111/jcmm.16976] PubMed: 34626063

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.