Tyrphostin 47A potent inhibitor of EGFR kinase activity

Tyrphostin 47 (CAS 122520-86-9)

Tyrphostin 47 | CAS 122520-86-9 is rated 5.0 out of 5 by 1.
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Synonym: RG-50864;Tyrphostin AG-213
Application: A potent inhibitor of EGFR kinase activity
CAS Number: 122520-86-9
Purity: >97%
Molecular Weight: 220.25
Molecular Formula: C10H8N2O2S
* Refer to Certificate of Analysis for lot specific data (including water content).
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Tyrphostin 47 is a protein tyrosine kinase inhibitor particularly potent against epidermal growth factor receptor (EGFR) kinase activity. Tyrphostin 47 has been observed to inhibit GTPase activity of transducin and the homologous insulin receptor kinase. It has also been found to also inhibit hyperactive motility of hamster spermatozoa. Tyrphostin 47 interferes with the proximal EGFR signaling pathway, causes G1-S transition arrest, and induces apoptosis in the human MCF-7 breast cancer cell line. In vero cell cultures, this product induced cell death and p38 MAPK phosphorylation.


References

1. Gazit, A., et al. 1989. J. Med. Chem. 32: 2344-2352. PMID: 2552117
2. Turbov, J.M., et al. 2002. J Surg Oncol. 79: 17-29. PMID: 11754373
3. Ikeda, M., et al. 2006. Eur. J. Pharmacol. 546: 36-39. PMID: 16919262
4. Mariappa, D., et al. 2006. Mol. Reprod. Dev. 73: 215-225. PMID: 16220544

Physical State :
Solid
Solubility :
Soluble in ethanol (20 mg/ml), DMSO (20 mg/ml), 1:1 DMSO:PBS (~0.5 mg/ml,pH 7.2), DMF (~15 mg/ml), and acetone.
Storage :
Store at -20° C
Melting Point :
175.04° C (Predicted)
Boiling Point :
~474.5° C at 760 mmHg (Predicted)
Density :
~1.5 g/cm3 (Predicted)
Refractive Index :
n20/D 1.78
IC50 :
EGFR: IC50 = 2.4 µM; PDGFR: IC50 = 3.5 µM; p210bcr-abl: IC50 = 5.9 µM; insulin receptor: IC50 = 640 µM; protein kinase C: IC50 = 60 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
5485187
MDL Number :
MFCD00133902
Beilstein Registry :
6508337
SMILES :
C\\1=CC(=O)C(=C/C1=C\\C(=C(\\N)/S)\\C#N)O

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Certificate of Analysis

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Tyrphostin 47  Product Citations

See how others have used Tyrphostin 47. Click on the entry to view the PubMed entry .

Citations 1 to 4 of 4 total

PMID: # 27872081  Guyett, PJ. et al. 2017. Antimicrob. Agents Chemother. 61:

PMID: # 12117110  Lorenzo, PL. et al. 2002. Equine Vet. J. 34: 378-382.

PMID: # 2788167  Lyall, RM. et al. 1989. J. Biol. Chem. 264: 14503-14509.

PMID: # 25715600  Ermakov, AM. et al. Biofizika. 59: 552-7.

Citations 1 to 4 of 4 total
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Rated 5 out of 5 by from Mariappa et al Mariappa et al. (PubMed ID 16220544) used the tyrosine kinase inhibitor, tyrphostin-47, to induce circular motility of hamster spermatozoa by significantly decreasing the phosphorylation of 45-60 kDa proteins. ' -SCBT Publication Review
Date published: 2015-07-18
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