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product name Tyrphostin 9


Description: Tyrphostin-9, also known as AG-17 or Malonoben, is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 460 µM in the human epidermoid carcinoma cell line A431. It also has inhibitory effect on the proliferation of SMC. Tyrphostin 9 potently inhibits the PDGF-dependent SMC proliferation with IC50 value of 40nM and inhibits the PDGF-dependent autophosphorylation of PDGFR with IC50 value of ~2.5μM. Besides that, Tyrphostin 9 also affects the phosphorylation of PLCγ (IC50 value of about 2.5μM) and the PDGF-dependent c-fos expression.

References: J Med Chem. 1989 Oct;32(10):2344-52; Proc Natl Acad Sci U S A. 2008 Aug 12;105(32):11218-23. 



Molecular Weight (MW)

282.38
Formula

C18H22N2O
CAS No.

10537-47-0
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 56 mg/mL (198.3 mM)
Water: <1 mg/mL
Ethanol: 56 mg/mL (198.3 mM)
Solubility (In vivo)

 
Synonyms

SF 6847, RG-50872, AG-17 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19417027

In Vitro

In vitro activity: SF 6847 inhibits the replication of herpes simplex virus type 1 (HSV-1) with IC50 of 40 nM. SF 6847 (50 nM) partly reverses sodium orthovanadate induced HSV-1 plaque formation. SF 6847 (< 400 nM) decreases the phosphorylation of viral phosphoproteins in a dose-dependent manner, but the SF 6847 (< 800 nM)-induced reduction of protein synthesis is not dose-dependent. SF 6847 prevents PDGF-induced tyrosine phosphorylation of LRP in caveolae in human fibroblasts suggesting that PDGF-BB-mediated LRP activation requires tyrosine phosphorylation and therefore activation of PDGFR-β. SF 6847 (1 mM) blocks the strain-induced stimulatory effect on DNA synthesis of fetal lung cells. SF 6847 (1 μM) causes increased exon inclusion of MAPT exon 10. SF 6847 does not affect the translation or stability of the two mRNAs. SF 6847 (1.6 μM) increases the inclusion of MAPT exon 10 by 2-fold in SHSY-5Y cells.


Kinase Assay


Cell Assay:

In Vivo  
Animal model  
Formulation & Dosage  
References J Med Chem. 1989 Oct;32(10):2344-52; Proc Natl Acad Sci U S A. 2008 Aug 12;105(32):11218-23. 

CFI-400946 (free base)

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Author: Sodium channel