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658403

Sigma-Aldrich

AG 538

A potent, cell-premeable, reversible, and competitive inhibitor of IGF-1 receptor kinase (IC₅₀ = 400 nM).

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Synonym(s):
AG 538, α-Cyano-(3,4-dihydroxy)cinnamoyl-(3ʹ,4ʹ-dihydroxyphenyl)ketone, Tyrphostin AG 538
Empirical Formula (Hill Notation):
C16HN11O5
CAS Number:
Molecular Weight:
427.25

Quality Level

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

dark orange to brown

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

−20°C

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572630658395T7697
AG 538 A potent, cell-premeable, reversible, and competitive inhibitor of IGF-1 receptor kinase (IC₅₀ = 400 nM).

658403

AG 538

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).

572630

SU5402

AG 18 A broad-spectrum protein tyrosine kinase inhibitor.

658395

AG 18

Sigma-Aldrich

T7697

I-OMe-Tyrphostin AG 538

form

solid

form

lyophilized solid

form

solid

form

solid

Quality Level

100

Quality Level

200

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

-

storage temp.

−20°C

storage temp.

2-8°C

storage temp.

−20°C

storage temp.

−20°C

solubility

DMSO: 5 mg/mL

solubility

DMSO: 25 mg/mL

solubility

DMSO: 100 mg/mL, ethanol: 50 mg/mL, acetic acid: soluble

solubility

DMSO: 50 mg/mL

General description

A potent, cell-premeable, reversible, and competitive inhibitor of IGF-1 receptor kinase (IC50 = 400 nM). Reaction is competitive with respect to IGF-1R substrate. Also inhibits the phosphorylation of PTK substrate poly(Glu,Tyr) by IGF-1R, IR, EGF-R, and Src (IC50 = 60 nM, 113 nM, 370 nM, and 2.4 µM, respectively). Inhibits the phosphorylation of PKB at a much higher concentration (IC50 = 76 µM).
A potent, cell-premeable, reversible, and competitive inhibitor of IGF-1R (insulin-like growth factor-1 receptor) kinase autophosphorylation (IC50 = 400 nM). Also inhibits the phosphorylation of PTK substrate poly (Glu,Tyr) by IGF-1R, IR, EGF-R, and Src (IC50 = 60 nM, 113 nM, and 2.4 µM respectively). Inhibits the phosphorylation of PKB at a much higher concentration (IC50 = 76 µM). Inhibition is competitive with respect to the substrate binding site of IGF-1R kinase. Also inhibits the authophosphorylation of IGF-1R and the activation of PKB and ERK2 in NIH-3T3 cells over-expressing IGF-1R.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
IGF-1 receptor kinase
Product competes with ATP.
Reversible: yes
Target IC50: 400 nM against IGF-1 receptor kinase

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Blum, G., et al. 2000. Biochemistry39, 15705.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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