572630
SU-5402
≥95% (HPLC), lyophilized solid, FGFR1 inhibitor, Calbiochem
Synonym(s):
SU5402, 3-[3-(2-Carboxyethyl)-4-methylpyrrol-2-methylidenyl]-2-indolinone
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About This Item
Empirical Formula (Hill Notation):
C17H16N2O3
CAS Number:
Molecular Weight:
296.32
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
product name
SU5402, SU5402, CAS 215543-92-3, is a cell-permeable, reversible, and ATP-competitive inhibitor of the tyrosine kinase activity of FGFR1 (IC₅₀ = 10-20 µM in the presence of 1 mM ATP).
Quality Level
Assay
≥95% (HPLC)
form
lyophilized solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
solubility
DMSO: 25 mg/mL
shipped in
ambient
storage temp.
2-8°C
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-
InChI key
JNDVEAXZWJIOKB-JYRVWZFOSA-N
General description
A cell-permeable, reversible, and ATP-competitive inhibitor of the tyrosine kinase activity of FGFR1 (IC50 = 10-20 µM in the presence of 1 mM ATP) by interacting with the catalytic domain of FGFR1. Also inhibits aFGF-induced phosphorylation of ERK1 and ERK2 (IC50 = 10-20 µM). In contrast to SU4984, it acts only as a weak inhibitor of tyrosine phosphorylation of the PDGF receptor. Does not inhibit the phosphorylation of insulin receptor and exhibits no inhibitory effect on EGF receptor kinase.
A cell-permeable, reversible, and ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth factor receptor 1 (FGFR1; IC50 = 10-20 µM in the presence of 1 mM ATP). Also inhibits aFGF-induced tyrosine phosphorylation of ERK1 and ERK2 (IC50 = 10-20 µM). In contrast to SU4984 (Cat. No. 572625), SU5402 is only a weak inhibitor of tyrosine phosphorylation of the PDGF receptor and does not inhibit phosphorylation of the insulin receptor. Does not inhibit the kinase activity of the EGF receptor. A 10 mM (500 µg/169 µl) solution of SU5402 (Cat. No. 572631) in DMSO is also available.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Fibroblast growth factor receptor 1 (FGFR1)
Fibroblast growth factor receptor 1 (FGFR1)
Product competes with ATP.
Reversible: yes
Target IC50: 10-20 &10-20 µM for fibroblast growth factor receptor 1 (FGFR1) in the presence of 1 mM ATP;M against FGFR1 in the presence of 1 mM ATP; 10-20 µM against inhibits aFGF-induced tyrosine phosphorylation of ERK1 and ERK2
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Mohammadi, M., et al. 1997. Science 276, 955.
Legal Information
Not available for sale in the United States.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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