SU 5402

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Cat.No. 3300 - SU 5402 | C17H16N2O3 | CAS No. 215543-92-3
Description: Potent FGFR and VEGFR inhibitor
Chemical Name: 2-[(1,2-Dihydro-2-oxo-3H-indol-3-ylidene)methyl]-4-methyl-1H-pyrrole-3-propanoic acid
Purity: ≥95% (HPLC)
Datasheet
Citations (12)
Literature

Biological Activity

Potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor (IC50 values are 0.02, 0.03, 0.51 and > 100 μM at VEGFR2, FGFR1, PDGFRβ and EGFR respectively). Inhibits embryonic left-right determination and exhibits potent anticancer activity in vitro and in vivo. Also attenuates integrin β4-induced differentiation of neural stem cells.

Technical Data

M. Wt 296.32
Formula C17H16N2O3
Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 215543-92-3
PubChem ID 5289418
InChI Key JNDVEAXZWJIOKB-JYRVWZFOSA-N
Smiles CC1=CNC(\C=C(C2=CC=CC=C2N3)/C3=O)=C1CCC(O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 29.63 100

Preparing Stock Solutions

The following data is based on the product molecular weight 296.32. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.37 mL 16.87 mL 33.75 mL
5 mM 0.67 mL 3.37 mL 6.75 mL
10 mM 0.34 mL 1.69 mL 3.37 mL
50 mM 0.07 mL 0.34 mL 0.67 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Sun et al (1999) 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. 42 5120 PMID: 10602697

Paterson et al (2004) Preclinical studies of fibroblast growth factor receptor 3 as a therapeutic target in multiple myeloma. Br.J.Haematol. 124 595 PMID: 14871245

Tanaka et al (2005) FGF-induced vesicular release of sonic hedgehog and retinoic acid in leftward nodal flow is critical for left-right determination. Nature 435 172 PMID: 15889083

Su et al (2009) Neural stem cell differentiation is mediated by integrin beta4 in vitro. Int.J.Biochem.Cell Biol. 41 916 PMID: 18834954


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Keywords: Potent VEGFR FGFR inhibitors inhibits Vascular Endothelial Growth Factor Receptors KDR Flt Receptor Tyrosine Kinases RTKs Fibroblast SU5402 neural stem cells differentiation FGFR

12 Citations for SU 5402

Citations are publications that use Tocris products. Selected citations for SU 5402 include:

Rodrigues (2017) Integration of Shh and Fgf signaling in controlling Hox gene expression in cultured limb cells. PNAS 114 3139 PMID: 28270602

Cunningham et al (2015) Retinoic Acid Activity in Undifferentiated Neural Progenitors Is Sufficient to Fulfill Its Role in Restricting Fgf8 Expression for Somitogenesis. PLoS One 10 e0137894 PMID: 26368825

Benzina et al (2015) A kinome-targeted RNAi-based screen links FGF signaling to H2AX phosphorylation in response to radiation. PLoS One 72 3559 PMID: 25894690

Neugebauer and Yost (2014) FGF signaling is required for brain left-right asymmetry and brain midline formation. Dev Biol 386 123 PMID: 24333178

Dai et al (2014) Calcium deficiency-induced and TRP channel-regulated IGF1R-PI3K-Akt signaling regulates abnormal epithelial cell proliferation. Cell Death Differ 21 568 PMID: 24336047

Bernet et al (2014) p38 MAPK signaling underlies a cell-autonomous loss of stem cell self-renewal in skeletal muscle of aged mice. Dev Biol 20 265 PMID: 24531379

Dean et al (2014) Dbx1b defines the dorsal habenular progenitor domain in the zebrafish epithalamus. Stem Cell Res Ther 9 20 PMID: 25212830

Hashiguchi and Mullins (2013) Anteroposterior and dorsoventral patterning are coordinated by an identical patterning clock. Development 140 1970 PMID: 23536566

Borroto-Escuela et al (2012) The existence of FGFR1-5-HT1A receptor heterocomplexes in midbrain 5-HT neurons of the rat: relevance for neuroplasticity. J Neurosci 32 6295 PMID: 22553035

Rankin et al (2012) Suppression of Bmp4 signaling by the zinc-finger repressors Osr1 and Osr2 is required for Wnt/β-catenin-mediated lung specification in Xenopus. Cell Mol Life Sci 139 3010 PMID: 22791896

Sato et al (2011) FGF8 signaling is chemotactic for cardiac neural crest cells. Neural Dev 354 18 PMID: 21419761

Tan et al (2011) Generation of trophoblast stem cells from rabbit embryonic stem cells with BMP4. Nat Med 6 e17124 PMID: 21359200


Do you know of a great paper that uses SU 5402 from Tocris? If so please let us know.

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Stem Cells

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

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Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

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Pathways for SU 5402

Protocols

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