Chemical Name: 5,6-Diphenyl-N-[[(2S)-tetrahydro-2-furanyl]methyl]furo[2,3-d]pyrimidin-4-amine
Biological ActivityAIM 100 is a potent Ack1 (TNK2) inhibitor (IC50 = 22 nM). Exhibits selectivity for Ack1 over ABL1, BTK, Lck and LYN; exhibits no inhibition of 25 other kinases. Suppresses phosphorylation of Tyr267 of the androgen receptor in prostate cancer cells. Also suppresses growth of radioresistant castration-resistant prostate cancer in xenograft tumors in mice. Also promotes DAT endocytosis and oligomerization.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Ack1-mediated androgen receptor phosphorylation modulates radiation resistance in castration-resistant prostate cancer.
Mahajan K, Coppola D, Rawal B et al.
J Biol Chem
Effect of Ack1 tyrosine kinase inhibitor on ligand-independent androgen receptor activity.
Mahajan et al.
Small molecule induced oligomerization, clustering and clathrin-independent endocytosis of the dopamine transporter.
Sorkina et al.
Citation for AIM 100
The citations listed below are publications that use Tocris products. Selected citations for AIM 100 include:
1 Citation: Showing 1 - 1
Ceritinib Enhances the Efficacy of Trametinib in BRAF/NRAS-Wild-Type Melanoma Cell Lines.
Authors: Verduzco Et al.
Mol Cancer Ther 2018;17:73
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