SU-5402


Catalog No. size PriceQuantity
M6536-2 2mg solid $95
M6536-10 10mg solid $401

Description

Cas:215543-92-3

Product Information:

SU-5402 is a 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 μ M at VEGFR2, FGFR1, PDGFR β and EGFR respectively).

 

Chemical Formula: C17H16N2O3

 

Exact Mass: 296.11609

 

Molecular Weight: 296.32054

 

Elemental Analysis: C, 68.91; H, 5.44; N, 9.45; O, 16.20

 

Synonym: 

 

SU5402

SU-5402

SU 5402

 

Chemical Name:

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

 

InChi Key:

JNDVEAXZWJIOKB-JYRVWZFOSA-N

 

InChi Code: I

nChI=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-

 

Smiles Code:

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

 

 

Technical Data:

 

Appearance: Orange solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro:

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. 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.

 

In Vivo

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). 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).

 

 

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.

 

  1. 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.

 

  1. 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.

 

  1. 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.

 

  1. 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.

 

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