Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC50 of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC50 of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity [1] [2] [3].

Tyrphostin AG 879 (AG 879, AG879)是酪氨酸激酶抑制剂，具有潜在抗癌活性，能够抑制TrKA磷酸化（IC 50 为10 μM），但对TrKB和TrKC无影响。 此外， Tyrphostin AG 879 也被广泛用作 HER2/ErbB2 的选择性抑制剂（ IC 50 为 1 μM ），比对 EGFR 和 PDGFR 的选择性高 100-500 倍。

Tyrphostin AG 879 is a compound that selectively inhibits protein tyrosine kinase and nerve growth factor-dependent tyrosine phosphorylation. (NCI) AG879? Follow these links to do a live 2D search or do a live 3D search for this compound, sorted by annotation score.

AG 879, in combination of PP1 (an inhibitor specific for Src kinase family), suppresses almost completely the growth of RAS-induced sarcomas in nude mice. In this paper we demonstrate that AG 879 even at 10 nM blocks the specific interaction between the Tyr-kinase ETK and PAK1 (a CDC42/ Rac-dependent Ser/Thr kinase) in cell culture.

AG 879, a TrkA inhibitor, kills cancer cells by inhibiting phosphorylation of NGFR, which inhibits subsequent signaling cascades and prevents neurite outgrowth, cell proliferation, and invasion4.

AG-879: A non-<wbr/>specific tyrphostin ErbB2 inhibitor. CAS Number: 148741-30-4. Synonym: Tyrphostin AG-879. Purity: ≥95%.

Tyrphostin AG 879有效抑制 HER2/ErbB2， IC50 为1 μM，作用于ErbB2比作用于PDGFR和EGFR选择性高100到500倍。 AG879浓度依赖性抑制FET6αS26X细胞的生长。 [1] AG879 (10 nM)阻断PAK1的活化，并抑制RAS诱导的NIH 3T3细胞癌变。 AG879 (<1 μM)抑制v-Ha-RAS转化的NIH 3T3成纤维细胞中ERK的Tyr磷酸化，以及ERK与PAK1的联合。 [2] AG 879剂量依赖性减少MCF-7细胞数量，并在0.4 mM下通过抑制DNA合成和有丝分裂，已经显示出显著的作用。 AG …

Key results: Tyrphostin AG879 selectively and dose-dependently inhibited Kv 4.2 and Kv 4.3 channels. In Kv 4.2/KChIP2 channels, AG879 induced prominent acceleration of the inactivation rate, use-dependent block and slowed the recovery from inactivation.

Tyrphostin AG 879 (AG879) has been used for studying its effect on ErbB2 receptor phosphorylation in A431 cells. This study reported that AG879 at 10 muM can cause 15% inhibition of receptor phosphorylation 1.AG879 has also been used as a neurotrophic tyrosine kinase receptor inhibitor to study the disruption of Sertoli cell aggregation 2.