product name Tyrphostin AG 879
Description: Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR. AG-879 is a tyrphostin compound that inhibits nerve growth factor-dependent TrkA tyrosine phosphorylation in PC-12 cells, HER2-ErbB2 kinase in several breast and ovarian cancer cell lines, and the VEGF receptor FLK1. It decreases cellular proliferation in human muscular sarcoma cell lines.
References: Cancer Res. 2005 Jul 1;65(13):5848-56; Anticancer Drugs. 2006 Sep;17(8):929-41.
316.46
Formula
C18H24N2OS
CAS No.
148741-30-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 36 mg/mL (113.7 mM)
Water: <1 mg/mL
Ethanol: 3 mg/mL (9.5 mM)
Solubility (In vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
Synonyms
AG 879
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/1942642
| In Vitro |
In vitro activity: 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). Kinase Assay: Cell Assay: MCF-7 cells are grown in 96-well plates containing 100 μL medium per well. Ten microliters of MTT solution (5 mg/ml in PBS) is added to each well and incubation continued for 4 h at 37 °C. Subsequently, 100 μL 10% SDS in 0.01 M HCl is added. After incubation at 37°C overnight, absorption is measured at 550 nm in an ELISA reader using a reference filter of 690 nm. |
|---|---|
| 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. |
| Animal model | Nude mice bearing v-Ha-RAS transformed NIH 3T3 cells |
| Formulation & Dosage | Dissolved in 30% DMSO with PBS; 20 mg/kg; i.p. injection |
| References | Cancer Res. 2005 Jul 1;65(13):5848-56; Anticancer Drugs. 2006 Sep;17(8):929-41. |
