Tyrphostin AG 99 A potent, cell-permeable and reversible inhibitor of EGFR and EGF-dependent cell proliferation

Tyrphostin AG 99 (CAS 118409-59-9)

Tyrphostin AG 99 | CAS 118409-59-9 is rated 5.0 out of 5 by 1.
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Synonym: Tyrphostin A46; Tyrphostin 46; AG 99; (E)-2-Cyano-3-(3,4-dihydroxyphenyl)-2-propenamide
Application: A potent, cell-permeable and reversible inhibitor of EGFR and EGF-dependent cell proliferation
CAS Number: 118409-59-9
Purity: >98%
Molecular Weight: 204.18
Molecular Formula: C10H8N2O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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Tyrphostin AG 99 is a potent, cell-permeable, reversible inhibitor of EGFR (epidermal growth factor receptor) and EGF-dependent cell proliferation. Stimulation of EGFRs result in tumor growth and proliferation, inhibition of apoptosis, stimulation of angiogenesis and the promotion of tissue invasion and metastasis. Tyrphostin AG 99 has been shown to inhibit EGFR phosphorylation and ERK1 and ERK2 activities.


References

1. Gazit, A., et al. 1989. J. Med. Chem. 32: 2344-2352. PMID: 2552117
2. Gazit, A., et al. 1991. J. Med. Chem. 34: 1896-1907. PMID: 1676428
3. Martin, B.L. 1998. Biochem. Pharmacol. 56: 483-488. PMID: 9763224
4. Pai, R., et al. 1998. Gastroenterology. 114: 706-713. PMID: 9516391
5. Ancha, H.R., et al. 2006. Dig. Dis. Sci. 51: 274-281. PMID: 16534669

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), ethanol (5 mM), DMF (~20 mg/ml), and 1:1 solution of DMSO:PBS (pH 7.2) us (~0.5 mg/ml). Insoluble in water.
Storage :
Store at -20° C
Melting Point :
188.96° C (Predicted)
Boiling Point :
~544.4° C at 760 mmHg (Predicted)
Density :
~1.5 g/cm3 (Predicted)
Refractive Index :
n20D 1.71 (Predicted)
IC50 :
EGFR: IC50 = 4 µM (human); Neu: IC50 = 6.4 µM (human); Lck: IC50 = 7 µM (human); Epidermal growth factor receptor (EGFR) kinase: IC50 = 10 µM; HIV-1 : IC50 = >100 µM (human)
Ki Data :
EGFR: Ki= 3.5 µM
pK Values :
pKa: 8.81 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
5328768
MDL Number :
MFCD00133901
SMILES :
C1=CC(=C(C=C1/C=C(\\C#N)/C(=O)N)O)O

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Pai et al Pai et al. (PubMed ID 9516391) found that Tyrphostin AG 99 significantly inhibited ulcer healing and reduced EGF-R levels, EGF-R phosphorylation, and ERK1 and ERK2 activity in rats. -SCBT Publication Review
Date published: 2015-07-13
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