ChemicalBook CAS DataBase List 149092-50-2

149092-50-2

Name	AG 825
CAS	149092-50-2
Molecular Formula	C19H15N3O3S2
MDL Number	MFCD01074971
Molecular Weight	397.47
MOL File	149092-50-2.mol

Chemical Properties

storage temp.	−20°C
solubility	DMSO: soluble
form	Yellow solid
color	Light yellow to yellow
Sensitive	Light Sensitive

Safety Data

Safety Statements	22-24/25 less more
WGK Germany	3

Hazard Information

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 Detail

Supplier

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