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Key Documents

572630

Sigma-Aldrich

SU-5402

≥95% (HPLC), lyophilized solid, FGFR1 inhibitor, Calbiochem

Synonyma:

SU5402, 3-[3-(2-Carboxyethyl)-4-methylpyrrol-2-methylidenyl]-2-indolinone

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About This Item

Empirický vzorec (Hillův zápis):
C17H16N2O3
Číslo CAS:
215543-92-3
Molekulová hmotnost:
296.32
MDL number:
MFCD08235144
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

200

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)
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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

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