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Tyrphostin 47 (CAS 122520-86-9)

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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 :

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

Rated 5 out of 5 by MC 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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Tyrphostin 47 (CAS 122520-86-9)

QUICK LINKS

References

Download SDS (MSDS)

Certificate of Analysis

Tyrphostin 47 Product Citations

Tyrphostin 47 (CAS 122520-86-9)

QUICK LINKS

References

Download SDS (MSDS)

Certificate of Analysis

Tyrphostin 47 Product Citations

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