AG879|cas 148741-30-4|DC Chemicals

Cas No.:	148741-30-4
Chemical Name:	Tyrphostin AG 879
Synonyms:	2-Propenethioamide,3-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-, (2E)-;Tyrphostin AG 879;(E)-3-amino-2-[(3,5-ditert-butyl-4-oxocyclohexa-2,5-dien-1-ylidene)methyl]-3-sulfanylprop-2-enenitrile;AG 879;AG 879 (Tyrphostin AG 879);AG-879;2-Propenethioamide,3-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-,(2E);BMK1-D4;Lopac-T-2067;α-Cyano-(3,5-di-t-butyl-4-hydroxy)thiocinnamide;(E)-3-[3,5-Bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-2-propenethioamide;TYRPHOSTIN 879;ALPHA-CYANO-(3,5-DI-T-BUTYL-4-HYDROXY)THIOCINNAMIDE;(3,5-DI-T-BUTYL-4-HYDROXYBENZYLIDENE)THIOCYANOACETAMIDE;ALPHA-CYANO-(3,5-DI-TERT-BUTYL-4-HYDROXY)THIOCINNAMAMIDE;2-CYANO-3-(3,5-DI-TERT-BUTYL-4-HYDROXYPHENYL)PROP-2-ENETHIOAMIDE;(E)-2-Cyano-3-(3,5-di-tert-butyl-4-hydroxyphenyl)prop-2-enethioamide;AG879;C18H24N2OS;(2E)-2-cyano-3-(3,5-di-tert-butyl-4-hydroxyphenyl)prop-2-enethioamide;tyrphostin AG879;BiomolKI_000028;BiomolKI2_000036;Lopac0_001175;BSPBio_001398;tyrphosti
SMILES:	N#C\C(C(N)=S)=C/C1=CC(C(C)(C)C)=C(O)C(=C1)C(C)(C)C
Formula:	C₁₈H₂₄N₂Os
M.Wt:	316.4610
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	TyrphostinAG879 is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation, but not TrKB and TrKC.[1] also a ErbB2 kinase inhibitor, has at least 500-fold higher selectivity to ErbB2 (IC50 = 1 μmol/L) than EGFR (IC50 >500 μmol/L).
Target:	TrKA [1], ErbB2 [2].IC 50: ErbB2 1 μmol/L [2].
In Vivo:	Treatment with TyrphostinAG879 in immunodepressed mice graft with leiomyosarcoma or promyelocytic leukemia cells result in dramatic reductions in tumor sizes. [1]
In Vitro:	TyrphostinAG879 significantly inhibit the A-type potassium currents in the cultured hippocampus neurons.[2] TyrphostinAG879 can reduce gephyrin puncta in GABAergic neurons and PSD-95 puncta in glutamatergic neurons where ErbB4 expression was low. [3]
References:	[1]. Rende M et al. Role of nerve growth factor and its receptors in non-nervous cancer growth: efficacy of a tyrosine kinase inhibitor (AG879) and neutralizing antibodies antityrosine kinase receptor A and antinerve growth factor: an in-vitro and in-vivo study. Anticancer Drugs. 2006 Sep;17(8):929-41. [2]. 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 Jan 1;66(1):404-11. [3]. Ting AK et al. Neuregulin 1 promotes excitatory synapse development and function in GABAergic interneurons. J Neurosci. 2011 Jan 5;31(1):15-25.

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