An inhibitor of ErbB3 (IC50 = 23 nM); binds to ErbB2

TX1-85-1 – 5 mg

Brand:
Cayman
CAS:
1603845-32-4
Storage:
-20
UN-No:
Non-Hazardous - /

TX1-85-1 is an inhibitor of the epidermal growth factor receptor tyrosine kinase ErbB3 (IC50 = 23 nM).{27814} It also binds to ErbB2, Lyn, and several other Src family kinases in a live cell chemical proteomics assay when used at a concentration of 2 µM. TX1-85-1 inhibits phosphorylation of Akt and ERK1/2 in ErbB3-dependent HCC2935 and OVCAR-8 cells when used at concentrations of 5 and 2 µM, respectively. However, it does not inhibit proliferation of ErbB3-dependent PC9 GR4, HCC827 GR8, or OVCAR-8 cells (EC50s = ≥10 µM).  

 

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Description

An inhibitor of ErbB3 (IC50 = 23 nM); binds to ErbB2, Lyn, and several other Src family kinases at 2 µM; inhibits phosphorylation of Akt and ERK1/2 in ErbB3-dependent HCC2935 and OVCAR-8 cells at 5 and 2 µM, respectively; does not inhibit proliferation of ErbB3-dependent PC9 GR4, HCC827 GR8, or OVCAR-8 cells (EC50s = ≥10 µM)

Formal name: N-[5-[1-[4-(4-acetyl-1-piperazinyl)cyclohexyl]-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-2-phenoxyphenyl]-2-propenamide

Synonyms: 

Molecular weight: 580.7

CAS: 1603845-32-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cancer|Cell Signaling|SRC Family Signaling||Research Area|Cell Biology|Cell Signaling|Growth Factor Receptors

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