PLX647|FMS/KIT Dual Kinase Inhibitor|DC Chemicals

PLX647|FMS/KIT Dual Kinase Inhibitor|DC Chemicals 
PLX647 is a potent and specific dual inhibitor of the receptor tyrosine kinases FMS and KIT.

Catlog: DC8157| Product name: PLX-647| Cas: 873786-09-5| Other names: PLX 647,PLX-647,PLX647| Molecule Formula: C21H17F3N4| MW: 382.38. Purity: >98%

Price: 100mg: 500 USD; 250mg: 900 USD; 1000mg: 1600 USD

A cell-permeable and bio-available azaindolylmethylpyridamine derivative that acts as a potent inhibitor against FMS and KIT (IC50 = 28 and 16 nM, respectively) by targeting the kinases in their inactive DGF-out conformation, while being less effective against Flt3, KDR/VEGFR2, CDC2L6/CDK11/CDK19, NTRK3/TrkC, DDR2, CDK8/cyclin C (IC50 = 91, 130, 350, 620, 700, and 710 nM, respectively) and exhibiting much reduced or little potency toward other kinases in a 400-kinase panel study (IC50 >1 µM). Shown to effectively inhibit cellular FLT3-ITD, FMS, KIT phosphorylations (IC50 from 20 to 250 nM), as well as FLT3-ITD-, FMS-, KIT-dependent proliferations (IC50 from 92 to 380 nM). Exhibits in vivo efficacy in several murine inflammation models (20 to 80 mg/kg b.i.d.; p.o.) and in preventing rat MRMT-1 breast carcinoma bone metastases-caused osteolysis (30 mg/kg b.i.d.; p.o.).

For research and scientific purpose only, not for human use.