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572630

Sigma-Aldrich

SU-5402

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

Sinônimo(s):

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

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About This Item

Fórmula empírica (Notação de Hill):
C17H16N2O3
Número CAS:
Peso molecular:
296.32
Número MDL:
Código UNSPSC:
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).

Nível de qualidade

Ensaio

≥95% (HPLC)

forma

lyophilized solid

fabricante/nome comercial

Calbiochem®

condição de armazenamento

OK to freeze
protect from light

solubilidade

DMSO: 25 mg/mL

Condições de expedição

ambient

temperatura de armazenamento

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-

chave InChI

JNDVEAXZWJIOKB-JYRVWZFOSA-N

Descrição geral

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.

Ações bioquímicas/fisiológicas

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

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Outras notas

Mohammadi, M., et al. 1997. Science 276, 955.

Informações legais

Not available for sale in the United States.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 1

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable


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H J Standley et al.
Development (Cambridge, England), 128(8), 1347-1357 (2001-03-23)
The community effect is an interaction among a group of many nearby precursor cells, necessary for them to maintain tissue-specific gene expression and differentiate co-ordinately. During Xenopus myogenesis, the muscle precursor cells must be in group contact throughout gastrulation in
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How human FGFR1 localizes to the PM is unknown. Currently, it is assumed that newly synthesized FGFR1 is continuously delivered to the PM. However, evidence indicates that FGFR1 is mostly sequestered in intracellular post-Golgi vesicles (PGVs) under normal conditions. In
Alejandro Gil-Gálvez et al.
Proceedings of the National Academy of Sciences of the United States of America, 119(11), e2114802119-e2114802119 (2022-03-10)
SignificanceIn this manuscript, we address an essential question in developmental and evolutionary biology: How have changes in gene regulatory networks contributed to the invertebrate-to-vertebrate transition? To address this issue, we perturbed four signaling pathways critical for body plan formation in

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