ChemicalBook--->CAS DataBase List--->149092-50-2

149092-50-2

149092-50-2 Structure

149092-50-2 Structure
IdentificationBack Directory
[Name]

AG 825
[CAS]

149092-50-2
[Synonyms]

AG 825
Zinc02572484
TYRPHOSTIN C15
AG 825 USP/EP/BP
TYRPHOSTIN AG 825
AG 825 (Tyrphostin AG 825)
AG 825 - CAS 149092-50-2 - Calbiochem
4-HYDROXY-3-METHOXY-5-(BENZOTHIAZOLYLTHIOMETHYL)BENZYLIDENECYANOACETAMIDE
5-[(BENZTHIAZOL-2-YL)THIOMETHYL]-4-HYDROXY-3-METHOXYBENZYLIDENECYANOACETAMIDE
5-[(BENZOTHIAZOL-2-YL)THIOMETHYL]-4-HYDROXY-3-METHOXYBENZYL-IDENECYANOACETAMIDE
3-[3-[(2-Benzothiazolylthio)methyl]-4-hydroxy-5-methoxyphenyl]-2-cyano- 2-Propenamide
2-Propenamide, 3-[3-[(2-benzothiazolylthio)methyl]-4-hydroxy-5-methoxyphenyl]-2-cyano-
(E)-3-[3-[(2-BENZOTHIAZOLYTHIO)METHYL]-4-HYDROXY-5-METHOXYPHENYL]-2-CYANO-2-PROPENAMIDE
Tyrphostin C15, 5-[(Benzothiazol-2-yl)thiomethyl]-4-hydroxy-3-methoxybenzylidenecyanoacetamide
[Molecular Formula]

C19H15N3O3S2
[MDL Number]

MFCD01074971
[MOL File]

149092-50-2.mol
[Molecular Weight]

397.47
Chemical PropertiesBack Directory
[storage temp. ]

−20°C
[solubility ]

DMSO: soluble
[form ]

Yellow solid
[color ]

Light yellow to yellow
[Sensitive ]

Light Sensitive
Safety DataBack Directory
[Safety Statements ]

22-24/25
[WGK Germany ]

3
Hazard InformationBack Directory
[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 -20°C
Spectrum DetailBack Directory
[Spectrum Detail]

AG 825(149092-50-2)1HNMR
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