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Merck

658403

AG 538

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

Synonym(s):

AG 538, α-Cyano-(3,4-dihydroxy)cinnamoyl-(3ʹ,4ʹ-dihydroxyphenyl)ketone, Tyrphostin AG 538

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About This Item

Empirical Formula (Hill Notation):
C16HN11O5
CAS Number:
133550-18-2
Molecular Weight:
427.25
MDL number:
MFCD00080276
NACRES:
NA.77
UNSPSC Code:
12352200

Key Documents

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Product Name

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

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

Quality Level

100

Related Categories

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

Disclaimer

Toxicity: Standard Handling (A)

General description

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.

Other Notes

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

Packaging

Packaged under inert gas

Preparation Note

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

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

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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Global Trade Item Number

SKUGTIN
658403-5MGCN04055977261585

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