AG 825A selective ErbB2 (Neu) inhibitor and apoptosis inducer

AG 825 (CAS 149092-50-2)

AG 825 | CAS 149092-50-2 is rated 5.0 out of 5 by 1.
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Synonym: Tyrphostin C15
Application: A selective ErbB2 (Neu) inhibitor and apoptosis inducer
CAS Number: 149092-50-2
Purity: >98%
Molecular Weight: 397.47
Molecular Formula: C19H15N3O3S2
* Refer to Certificate of Analysis for lot specific data (including water content).
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AG 825 is shown to be a potent inhibitor of EGFR (epidermal growth factor receptor) and Neu (HER-2) kinases. Mechanistic studies report that this compound inhibits mitogenic signaling elements downstream to the growth receptor kinase. Studies indicate that inhibition of HER-2 causes imbalance between extracellular signal-regulated kinase 1/2 and p38 mitogen-activated protein kinase activation. It has also been observed that treatment of cells with AG 825 results in apoptosis induction and inhibition of colony formation.


References

1. Gazit, A., et al. 1993. J. Med. Chem. 36: 3556-3564. PMID: 7902440
2. Murillo, H., et al. 2001. Cancer Res. 61: 7408-7412. PMID: 11606371
3. Koval, J., et al. 2010. Photochem. Photobiol. 86: 200-205. PMID: 19912559

Physical State :
Solid
Solubility :
Soluble in DMSO (25 mg/ml), methanol, ethanol (~0.2 mg/ml), DMF (~30 mg/ml), and 1:3 solution of DMSO:PBS (pH 7.2) (~0.1 mg/ml).
Storage :
Store at -20° C
Melting Point :
282.33° C (Predicted)
Boiling Point :
689.27° C at 760 mmHg (Predicted)
Density :
1.48 g/cm3 (Predicted)
Refractive Index :
n20D 1.73 (Predicted)
IC50 :
HER1-2 tyrosine kinase : IC50 = 0.35 µM; EGFR: IC50 = 19 µM; PDGFR: IC50 = 40 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
5353392
MDL Number :
MFCD01074971
SMILES :
COC1=CC(=CC(=C1O)CSC2=NC3=CC=CC=C3S2)C=C(C#N)C(=O)N

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Hsu Hsu, FN. et al. (PubMed 21364123) found that AG 825 (Tyrphostin C15), an inhibitor of EGFR and HER-2 (Neu) kinases, more effectively caused androgen receptor (AR) degradation and diminished AR Ser(81) phosphorylation in androgen-independent prostate cancer cell lines compared to LNCaP cells. They conclude that Her2 plays an important role in the support of AR protein stability in the transition of androgen requirement in prostate cancer cells. -SCBT Publication Review
Date published: 2015-06-16
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