pexidartinib-hcl

Description: Pexidartinib HCl (formerly also know as PLX-3397 HCl) is a novel, orally bioavailable, potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib binds to and inhibits phosphorylation of stem cell factor receptor (KIT), colony-stimulating factor-1 receptor (CSF1R) and FMS-like tyrosine kinase 3 (FLT3), which may result in the inhibition of tumor cell proliferation and down-modulation of macrophages, osteoclasts and mast cells involved in the osteolytic metastatic disease. Pexidartinib is under development by Plexxikon for the treatment of tenosynovial giant cell tumors. It is in a phase 3 clinical trial for Pigmented Villonodular Synovitis (PVNS) or Giant Cell Tumor of the Tendon Sheath (GCT-TS)

References: Cancer Discov. 2011 Jun; 1(1):54-67; Mol Med. 2012 May 9; 18:519-27; Blood. 2012 Oct 11; 120(15):3126-35.

Related CAS: 2040295-03-0 (HCl); 2169310-71-6 (2HCl)