AG879 Inhibitor CAS No. 148741-30-4

Cat. No.	Name	Size	Price
KI0465	AG879	5 mg	$112
	AG879	10 mg	$176
	AG879	25 mg	$432

Chemical Characteristic

Product Name	AG879
CAS No.	148741-30-4
Molecular Weight	316.46
Formula	C₁₈H₂₄N₂OS
Chemical Name	(E)-3-[3,5-Bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-2-propenethioamide; AG 879
Smiles	C(=S)(/C(=C/c1cc(c(c(c1)C(C)(C)C)O)C(C)(C)C)/C#N)N
Chemical Structure

Biological activities

AG 879 is widely used specific Tyr kinase inhibitor for ErbB2 and FLK-1 (a VEGF receptor). AG 879 even at 10 nM inhibits the specific interaction between the Tyr-kinase ETK and PAK1 in v-Ha-RAS-transformed NIH 3T3 fibroblasts (RAS cells). Although the Tyr-kinases Src and FAK directly activate ETK, Src is insensitive to AG 879, and FAK is prevented by 100 nM AG 879, but not by 10 nM AG 879. 10 nM AG 879 strongly inhibits the activity of PAK1 kinase in RAS cells without affecting the levels of PAK1 protein. AG 879 also blocks the anchorage-independent growth of RAS cell in soft agar. AG 879 inhibited the large colony formation with an IC50 of 1-10 nM. AG 879 strongly prevents the Tyr-phosphorylation of PAK1 by ETK. The IC50 of AG 879 for ETK is 5 nM.^[1] Combination of AG1478 and AG879 led to synergistic effects. Synergistic prevention of AG1478 and AG879 was related with induction of apoptosis as reflected by poly (ADP-ribose) polymerase cleavage, caspase-3 activation, and Annexin V staining. The AG1478 and AG879 combination treatment generates 10.72% of the cells undergoing apoptosis. AG879 concentration-dependently prevented the phosphorylation of ErbB2 Y1139. ^[2] AG879 inhibited the activity of ErbB2 with an IC50 of 1 μM, with at least 500-fold higher selectivity than EGFR (IC50 >500 μM). The ErbB2-selective TKI AG879 at a concentration of 1 μM prevented activation of the ErbB2 Y1248 site. AG879 treatment upregulated phosphorylation at the EGFR Y1173 site.^[3] Combination of AG879 with PP1, which is an inhibitor specific for Src kinase family, prevents almost completely the growth of RAS-induced sarcomas in nude mice.^[1]

Protocols

AG879 was dissolved in DMSO to generate 20 mM stock solutions.^[2]

References

[1] He H, et al. The Tyr-kinase inhibitor AG879, that blocks the ETK-PAK1 interaction, suppresses the RAS-induced PAK1 activation and malignant transformation. Cancer Biol Ther. 2004 , 3(1): 96-101. [2] Zhou Y, et al. Synergy of epidermal growth factor receptor kinase inhibitor AG1478 and ErbB2 kinase inhibitor AG879 in human colon carcinoma cells is associated with induction of apoptosis. Cancer Res. 2005, 65(13): 5848-5856. [3] Zhou Y, et al. Blockade of EGFR and ErbB2 by the novel dual EGFR and ErbB2 tyrosine kinase inhibitor GW572016 sensitizes human colon carcinoma GEO cells to apoptosis. Cancer Res. 2006, 66(1): 404-411.

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