Pexidartinib (PLX3397; Turalio; CML261; FP113)

Description: Pexidartinib (formerly PLX-3397; CML-261; FP-113; trade name Turalio) is an orally bioavailable and multi-targeted RTK (receptor tyrosine kinase) inhibitor of CSF-1R, Kit, and Flt3 with potential antineoplastic activity. It inhibits CSF-1R, Kit, and Flt3 with IC50s of 20 nM, 10 nM and 160 nM, respectively. In August 2019, Pexidartinib received FDA approval for treatment of giant-cell tumor of the tendon sheath (GC-TS). However, it is available in the US only through the Turalio Risk Evaluation and Mitigation Strategy (REMS) Program.

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); 1029044-16-3 (free base); 2169310-71-6 (2HCl)

Chemical Name: 5-((5-chloro-1H-pyrrolo[2, 3-b]pyridin-3-yl)methyl)-N-((6-(trifluoromethyl)pyridin-3-yl)methyl)pyridin-2-amine

SMILES Code: FC(C1=CC=C(CNC2=NC=C(CC3=CNC4=NC=C(Cl)C=C43)C=C2)C=N1)(F)F