658425

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

Properties

• 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

Description

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

Safety Information

• Pictograms: GHS06
• Signal Word: Danger
• Hazard Statements: H301 + H311
• Precautionary Statements: P264 - P270 - P280 - P301 + P310 - P302 + P352 + P312 - P361 + P364
• Hazard Classifications: Acute Tox. 3 Dermal - Acute Tox. 3 Oral
• Storage Class Code: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable