AG 825

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Cat.No. 1555 - AG 825 | C19H15N3O3S2 | CAS No. 149092-50-2
Description: Selective ErbB2 inhibitor
Alternative Names: Tyrphostin AG 825
Chemical Name: (E)-3-[3-[2-Benzothiazolythio)methyl]-4-hydroxy-5-methoxyphenyl]-2-cyano-2-propenamide
Datasheet
Citations (4)
Literature

Biological Activity

Selective ErbB2 inhibitor (IC50 values are 0.15 and 19 μM at ErbB2 and ErbB1 respectively). Preferentially triggers p38 MAP kinase-dependent apoptosis in androgen-independent prostate cancer cells.

Technical Data

M. Wt 397.47
Formula C19H15N3O3S2
Storage Store at +4°C
CAS Number 149092-50-2
PubChem ID 6091659
InChI Key KXDONFLNGBQLTN-WUXMJOGZSA-N
Smiles COC1=CC(\C=C(/C#N)C(N)=O)=CC(CSC2=NC3=C(S2)C=CC=C3)=C1O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.75 100

Preparing Stock Solutions

The following data is based on the product molecular weight 397.47. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.52 mL 12.58 mL 25.16 mL
5 mM 0.5 mL 2.52 mL 5.03 mL
10 mM 0.25 mL 1.26 mL 2.52 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Gazit et al (1993) Tyrphostins. 3. Structure-activity relationship studies of α-substituted benzylidenemalononitrile 5-S-aryltyrphostins. J.Med.Chem. 36 3556 PMID: 7902440

Murillo et al (2001) Tyrphostin AG825 triggers p38 mitogen-activated protein kinase-dependent apoptosis in androgen-independent prostate cancer cells C4 and C4-21. Cancer Res. 61 7408 PMID: 11606371

Osherov et al (1993) Selective inhibition of the epidermal growth factor and HER2/Neu receptors by tyrphostins. J.Biol.Chem. 268 11134 PMID: 8098709


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4 Citations for AG 825

Citations are publications that use Tocris products. Selected citations for AG 825 include:

Lee et al (2014) Neuregulin autocrine signaling promotes self-renewal of breast tumor-initiating cells by triggering HER2/HER3 activation. Cancer Res 74 341 PMID: 24177178

Lucchetti et al (2013) The prolyl isomerase Pin1 acts synergistically with CDK2 to regulate the basal activity of estrogen receptor α in breast cancer. PLoS One 8 e55355 PMID: 23390529

Akhtar et al (2013) Activation of ErbB2 and Downstream Signalling via Rho Kinases and ERK1/2 Contributes to Diabetes-Induced Vascular Dysfunction. PLoS One 8 e67813 PMID: 23826343

Kedrin et al (2009) ERBB1 and ERBB2 have distinct functions in tumor cell invasion and intravasation. Clin Cancer Res 15 3733 PMID: 19458057


Do you know of a great paper that uses AG 825 from Tocris? If so please let us know.

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