Chemical Name: 5,6-Diphenyl-N-[[(2S)-tetrahydro-2-furanyl]methyl]furo[2,3-d]pyrimidin-4-amine
Biological ActivityPotent 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.
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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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Combined pharmacological inhibition of MEK and ACK1 suppresses long-term growth of WM209 and SK-MEL-23 cells.