[CAS NO. 148741-30-4] Tyrphostin AG 879

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PRODUCTS SPECIFICATIONS [148741-30-4]

Catalog

SLK-S2816

Brand

Selleck

CAS

148741-30-4

DESCRIPTION [148741-30-4]

Overview

MDL	MFCD00236450
Molecular Weight	316.46
Molecular Formula	C18H24N2OS
SMILES	C(C)(C)(C)C1=C(O)C(C(C)(C)C)=CC(/C=C(/C(N)=S)\C#N)=C1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	3.1600 mL	15.7998 mL	31.5996 mL
5 mM	0.6320 mL	3.1600 mL	6.3199 mL
10 mM	0.3160 mL	1.5800 mL	3.1600 mL
50 mM	0.0632 mL	0.3160 mL	0.6320 mL

Description

Tyrphostin AG 879 potently inhibits with of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.

Targets

HER2-Neu ^[6] (Cell-free assay)	Trk ^[6] (Cell-free assay)
1.0 μM	10 μM

In vitro

AG879 inhibits growth of FET6αS26X cells in a concentration-dependent manner. AG879(10 nM) blocks the activation of PAK1 and suppresses RAS-induced malignant transformation of NIH 3T3 cells. AG879(<1 μM) inhibits the Tyr-phosphorylation of ERK and its association with PAK1 in v-Ha-RAS-transformed NIH 3T3 fibroblasts. AG 879 dose-dependently reduce MCF-7 cell numbers and show already a significant effect at 0.4 mM through inhibiting DNA synthesis and mitotic. AG 879(<20 μM) inhibits activation of ERK-1/2 in MCF-7 cell. AG 879(5 μM) decreases expression of Hsp90 client proteins RAF-1 and HER-2. AG879(20 μM) dramatically decreases proliferation with a variable increase in apoptosis in Cell lines from human leiomyosarcoma (HTB-114, HTB-115, HTB-88), rhabdomyosarcoma (HTB-82, TE-671), prostatic adenocarcinoma (PC-3), acute promyelocytic leukemia (HL-60) and histiocytic lymphoma (U-937).

In vivo

AG879(2 mg) induces a decrease in cancer growth in athymic NOD/SCID mice grafted with HTB-114 or HL-60. AG 879(20 mg/kg) treatment keeps 50% of mice absolutely free of RAS-induced sarcomas, and dramatically reduces the size of the growing sarcomas in the nude mice carrying v-Ha-RAS transformed NIH 3T3 cells.

References

[1] Zhou Y, et al. Cancer Res, 2005, 65(13), 5848-5856.
[2] He H, et al. Cancer Biol Ther, 2004, 3(1), 96-101.
[3] Larsson LI, et al. Cell Mol Life Sci, 2004, 61(19-20), 2624-2631.
[4] Rende M, et al. Anticancer Drugs, 2006, 17(8), 929-941.
[5] He H, et al. Cancer J, 2001, 7(3), 191-202.
[6] Levitzki A, et al. Science. 1995, 267(5205), 1782-1788.

Synonyms

2-Propenethioamide, 3-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-, (2E)-

2-Propenethioamide, 3-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-, (E)-

(2E)-3-[3,5-Bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-2-propenethioamide

AG 879

Tyrphostin AG 879