SU-5402 - FGFR inhibitor

SU-5402 is a potent inhibitor of FGFR, VEGFR, and PDGFR. SU-5402 has been used in many studies to inhibit cancer cell growth, or modulate stem cell phenotypes, including maintenance of mouse ESCs, or inducing generation of functional human nociceptors from human ESCs/iPSCs when combined with LDN193189/BMP inhibitor, SB431542/TGFβ inhibitor, CHIR99021/GSK3 inhibitor, and DAPT/Notch inhibitor.

Product information

CAS Number: 215543-92-3

Molecular Weight: 296.32

Formula: C17H16N2O3

Synonym:

SU5402

SU-5402

SU 5402

Related CAS Number:

210303-49-4 ((Z)-SU5402)

215543-92-3 ((EZ)-SU5402)

Chemical Name: 3-(4-methyl-2-((2-oxoindolin-3-ylidene)methyl)-1H-pyrrol-3-yl)propanoic acid.

Smiles: CC1=CNC(C=C2C3=CC=CC=C3NC2=O)=C1CCC(O)=O

InChiKey: JNDVEAXZWJIOKB-JYRVWZFOSA-N

InChi: InChI=1S/C17H16N2O3/c1-10-9-18-15(11(10)6-7-16(20)21)8-13-12-4-2-3-5-14(12)19-17(13)22/h2-5,8-9,18H,6-7H2,1H3,(H,19,22)(H,20,21)/b13-8-

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Solubility (25°C) DMSO: 59 mg/mL(199.1 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

SU5402 inhibits VEGF-, FGF-, PDGF- dependent cell proliferation with IC50 of 0.05 μM, 2.80μM, 28.4 μM, respectively. In HUVECs, SU5416 selectively inhibits VEGF-driven mitogenesis in a dose-dependent manner with IC50 of 0.04 μM. In nasopharyngeal epithelial cells, SU5402 attenuates LMP1-mediated aerobic glycolysis, cellular transformation, cell migration, and invasion. In mouse C3H10T1/2 cells, SU 5402 diminishes the effect of FGF23 on cell differentiation.

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.

References:

1. Hu X, Zhang P, Xu Z, Chen H, Xie X. GPNMB enhances bone regeneration by promoting angiogenesis and osteogenesis: potential role for tissue engineering bone. J Cell Biochem. 2013 Dec;114(12):2729-37. doi: 10.1002/jcb.24621. PubMed PMID: 23794283.
2. Nguyen TK, Tran VM, Sorna V, Eriksson I, Kojima A, Koketsu M, Loganathan D, Kjellén L, Dorsky RI, Chien CB, Kuberan B. Dimerized glycosaminoglycan chains increase FGF signaling during zebrafish development. ACS Chem Biol. 2013 May 17;8(5):939-48. doi: 10.1021/cb400132r. Epub 2013 May 7. PubMed PMID: 23614643.
3. Chang CH, Huang YL, Shyu MK, Chen SU, Lin CH, Ju TK, Lu J, Lee H. Sphingosine-1-phosphate induces VEGF-C expression through a MMP-2/FGF-1/FGFR-1-dependent pathway in endothelial cells in vitro. Acta Pharmacol Sin. 2013 Mar;34(3):360-6. doi: 10.1038/aps.2012.186. Epub 2013 Feb 4. PubMed PMID: 23377549.
4. Sun N, Zou H, Yang L, Morita K, Gong P, Shiba T, Akagawa Y, Yuan Q. Inorganic polyphosphates stimulate FGF23 expression through the FGFR pathway. Biochem Biophys Res Commun. 2012 Nov 16;428(2):298-302. doi: 10.1016/j.bbrc.2012.10.051. Epub 2012 Oct 18. PubMed PMID: 23085229.
5. Bojesen KB, Clausen O, Rohde K, Christensen C, Zhang L, Li S, Køhler L, Nielbo S, Nielsen J, Gjørlund MD, Poulsen FM, Bock E, Berezin V. Nectin-1 binds and signals through the fibroblast growth factor receptor. J Biol Chem. 2012 Oct 26;287(44):37420-33. doi: 10.1074/jbc.M112.345215. Epub 2012 Sep 5. PubMed PMID: 22955284; PubMed Central PMCID: PMC3481338.

Products are for research use only. Not for human use.