3-[(6,7-Dimethoxy-4-quinazolinyl)amino]-phenol

Inhibitor of IgE-mediated mast cell responses. Tau-Tubulin Kinase 1 inhibitor, phosphorylated TTBK1 KD = 0.46 µM, nonphosphorylated TTBK1 KD = 0.24 µM.

REarranged during Transfection (RET) kinase inhibitor, IC50 = 5 nM, KDR (VEGFR2) kinase inhibitor, IC50 = 66 nM

OTAVAchemicals Catalogue Number: 7015070102
CAS Registry Number: 211555-08-7
Purity: 97% (HPLC)

Ref.: Pharm. Res. 1999, 16, 1, 117 – 122 Chem. Med. Chem. 2013, 8, 1846 – 1854 Eur. J. Med. Chem. 2016, 112, 20 – 32

Abstract: WHI-P180 is an active inhibitor of IgE-mediated mast cell responses in vitro and in vivo. Inhibitor of neuron-specific tau-tubulin kinase 1 (TTBK1) is a serine/threonine/tyrosine kinase that putatively phosphorylates residues including Y197, S198, S199, S202 and S422 in tau protein. Hyperphosphorylation of tau protein is the primary cause of tau pathology and neuronal death associated with Alzheimer’s disease. RET and KDR (VEGFR2) kinase inhibitor,

DOI: 10.1023/a:1018835232027 10.1002/cmdc.201300274 10.1016/j.ejmech.2016.01.039