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658425

Sigma-Aldrich

AG 17

Anti-proliferative agent that acts as a selective inhibitor of the platelet-derived growth factor receptor tyrosine kinase (IC₅₀ = 500 nM).

Synonym(s):

AG 17, NSC 242557, 3,5-di- t-Butyl-4-hydroxy-benzylidenemalononitrile, α-Cyano-(3,5-di- t-butyl-4-hydroxy)cinnamonitrile, Tyrphostin A9, RG 50872

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About This Item

Empirical Formula (Hill Notation):
C18H22N2O
CAS Number:
10537-47-0
Molecular Weight:
282.38
MDL number:
MFCD00209853
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥99% (TLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

pale yellow

solubility

DMSO: 10 mg/mL
ethanol: 5 mg/mL

shipped in

ambient

storage temp.

−20°C

InChI

1S/C18H22N2O/c1-17(2,3)14-8-12(7-13(10-19)11-20)9-15(16(14)21)18(4,5)6/h7-9,21H,1-6H3

InChI key

MZOPWQKISXCCTP-UHFFFAOYSA-N

General description

A selective, cell-permeable, reversible, and substrate competitive inhibitor of the platelet-derived growth factor receptor tyrosine kinase (IC50 = 500 nM). Anti-proliferative agent. Uncoupler of oxidative phosphorylation. Induces apoptosis in vitro and cell growth arrest in NHL cell lines.
Anti-proliferative agent that acts as a selective inhibitor of the platelet-derived growth factor receptor tyrosine kinase (IC50 = 500 nM). A potent, cell-permeable, reversible, and substrate competitive inhibitor of TNF-induced tyrosine phosphorylation of PYK2. Uncouples oxidative phosphorylation and induces apoptosis and cell growth arrest in NHL cell lines. Inhibits Cdk2 activity in lymphoma cell lines.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Platelet-derived growth factor receptor tyrosine kinase
Product competes with ATP.
Reversible: yes
Target IC50: 500 nM against platelet-derived growth factor receptor tyrosine kinase

Warning

Toxicity: Toxic (F)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Other Notes

Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.
Fuortes, M., et al. 1999. J. Clin. Invest.104, 327.
Palumbo, G.A., et al. 1997. Cancer Res. 57, 2434.
Burger, A.M., et al. 1995. Cancer Res.55, 2794.
Palumbo, G.A., et al. 1994. Blood84, 296a.
Bilder, G.E., et al. 1991. Am. J. Physiol. 260, C721.
Levitzki, A., and Gilon, S. 1991. Trends Pharmacol. Sci. 12, 171.
Terada, H. 1981. Biochim. Biophys. Acta639, 225

Legal Information

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

pictograms

Skull and crossbones
GHS06

signalword

Danger

Hazard Classifications

Acute Tox. 3 Dermal - Acute Tox. 3 Oral

wgk_germany

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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