572630

SU-5402

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

• Synonym(s): SU5402, 3-[3-(2-Carboxyethyl)-4-methylpyrrol-2-methylidenyl]-2-indolinone
• Empirical Formula (Hill Notation): C₁₇H₁₆N₂O₃
• CAS Number: 215543-92-3
• Molecular Weight: 296.32
• MDL number: MFCD08235144
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• 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

Description

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable