AG 825
AG 825 Basic information
- Product Name:
- AG 825
- Synonyms:
-
- TYRPHOSTIN AG 825
- TYRPHOSTIN C15
- AG 825
- 5-[(BENZTHIAZOL-2-YL)THIOMETHYL]-4-HYDROXY-3-METHOXYBENZYLIDENECYANOACETAMIDE
- 5-[(BENZOTHIAZOL-2-YL)THIOMETHYL]-4-HYDROXY-3-METHOXYBENZYL-IDENECYANOACETAMIDE
- 4-HYDROXY-3-METHOXY-5-(BENZOTHIAZOLYLTHIOMETHYL)BENZYLIDENECYANOACETAMIDE
- 3-[3-[(2-Benzothiazolylthio)methyl]-4-hydroxy-5-methoxyphenyl]-2-cyano- 2-Propenamide
- Tyrphostin C15, 5-[(Benzothiazol-2-yl)thiomethyl]-4-hydroxy-3-methoxybenzylidenecyanoacetamide
- CAS:
- 149092-50-2
- MF:
- C19H15N3O3S2
- MW:
- 397.47
- Product Categories:
-
- Protein Kinase
- Mol File:
- 149092-50-2.mol
AG 825 Chemical Properties
- storage temp.
- −20°C
- solubility
- DMSO: soluble
- form
- Yellow solid
- color
- Light yellow to yellow
- Sensitive
- Light Sensitive
Safety Information
- Safety Statements
- 22-24/25
- WGK Germany
- 3
MSDS
- Language:English Provider:SigmaAldrich
AG 825 Usage And Synthesis
Uses
A selective ErbB2 inhibitor
Uses
AG 825 is a selective ErbB2 (Neu) inhibitor and apoptosis inducer.
Definition
ChEBI: An organic sulfide that consists of 1,3-benzothiazole-2-thiol in which the hydrogen attached to the sulfur atom is replaced by a 5-[(1E)-3-amino-2-cyano-3-oxoprop-1-en-1-yl]-2-hydroxy-3-methoxybenzyl group. It acts as an epidermal growth factor receptor antagonist.
Biological Activity
Selective ErbB2 inhibitor (IC 50 values are 0.15 and 19 mM at ErbB2 and ErbB1 respectively). Preferentially triggers p38 MAP kinase-dependent apoptosis in androgen-independent prostate cancer cells.
in vivo
AG-825 (20 mg/kg, i.p.) decreases peritoneal inflammation in Zymosan (HY-159069)-treated mice, and increases lung neutrophil apoptosis and macrophage efferocytosis in a murine acute lung injury model[4].
AG-825 (1 mg/kg, min-osmotic pump, 14 days) causes cardiac dilation and selective increase in β1AR density in mice[7].
| Animal Model: | Murine model of LPS induced acute lung inflammation[4] |
| Dosage: | 20 mg/kg |
| Administration: | Intraperitoneal injection (i.p.) |
| Result: | Had no effect on percentage of, or absolute number of neutrophils or macrophages. Increased the percentage of neutrophil apoptosis. Elevated macrophage efferocytosis. |
| Animal Model: | Murine model of Zymosan (HY-159069)-induced peritonitis[4] |
| Dosage: | 20 mg/kg |
| Administration: | Intraperitoneal injection (i.p.) |
| Result: | Did not induce leukopenia. Showed fewer inflammatory cells in peritoneal lavage. Reduced the neutrophil chemoattractant and proinflammatory cytokine, KC. Reduced IgM. |
IC 50
ErbB2: 0.35 μM (IC50); EGFR: 19 μM (IC50)
storage
Store at +4°C
AG 825Supplier
- Tel
- 821-50328103-801 18930552037
- 3bsc@sina.com
- Tel
- 0512-65856968
- sales@chireach.com
- Tel
- 0330-2528181
- sales@vdmbio.com
- Tel
- 021-021-021-67601398-809-809-809 15221380277
- marketing_china@spectrumchemical.com
- Tel
- +49 5662 408730
- info@synchem.de
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