PLX647|PLX 647,FMS/KIT inhibitor|DC Chemicals

PLX647|PLX 647,FMS/KIT inhibitor|DC Chemicals
PLX647 is a highly specific dual FMS/KIT kinase inhibitor with IC50 of 28/16 nM respectively.

Catlog: DC8107| Product name: PLX647| Cas: 873786-09-5| Other names: PLX 647,PLX-647| Molecule Formula: C21H17F3N4| MW: 382.38. Purity: >98%

Price: 100mg: 500 USD; 250mg: 900 USD; 1000mg: 1900 USD

PLX647 is a highly specific dual FMS/KIT kinase inhibitor with IC50 of 28/16 nM respectively.
IC50 value: 28/16 nM(FMS/KIT)
in vitro: PLX647 was tested against a panel of 400 kinases at a concentration of 1 μM, 35-fold above its FMS enzymatic IC50 and 60-fold above its KIT enzymatic IC50. In addition to FMS and KIT, the activities of only nine kinases were inhibited by more than 50%. PLX647 potently inhibits the growth of FLT3–ITD-expressing MV4-11 cells (IC50 = 0.11 μM) but not OCI-AML5 (IC50 = 1.6 μM), which express wild-type FLT3. PLX647 displayed minimal inhibition of the proliferation of Ba/F3 cells expressing BCR–KDR (IC50 = 5 μM) .
in vivo: PLX647 (40 mg/kg) was dosed orally 4.25 h before LPS injection. Treatment with PLX647 reduced serum TNF-α levels by 85% compared with the vehicle control. In the same experiment, the positive control dexamethasone (0.5 mg/kg, PO) lowered the TNF-α levels by 96%. Treatment with 40 mg/kg PLX647 also resulted in significant inhibition of IL-6 release (75%), with similar potency to dexamethasone (70%) . In the UUO kidneys, treatment with PLX647 [40 mg/kg twice daily (BID)] resulted in reduction in the levels of F4/80+ macrophages by 77% compared with vehicle.

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