Home Protein Tyrosine Kinase EGFR inhibitor Tyrphostin 9

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Tyrphostin 9 EGFR inhibitor

Cat.No.S2895

Tyrphostin 9 (SF 6847, RG-50872) is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM.
Tyrphostin 9 EGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 282.38

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Quality Control

Batch: S289501 DMSO]56 mg/mL]false]Ethanol]56 mg/mL]false]Water]Insoluble]false Purity: 99.99%
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99.99

Solubility

In vitro
Batch:

DMSO : 56 mg/mL (198.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 56 mg/mL

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 282.38 Formula

C18H22N2O

 Storage (From the date of receipt)
CAS No. 10537-47-0 Download SDF Storage of Stock Solutions

Synonyms SF 6847, RG-50872 Smiles CC(C)(C)C1=CC(=CC(=C1O)C(C)(C)C)C=C(C#N)C#N

Mechanism of Action

Targets/IC50/Ki
PDGFR
0.5 μM
EGFR
460 μM
In vitro
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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/7653578/
  • [5] https://pubmed.ncbi.nlm.nih.gov/18678901/
  • [6] https://pubmed.ncbi.nlm.nih.gov/2143901/

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