85-2072-93　FMS/KIT Dual Kinase Inhibitor, PLX647 (CDC2L6/CDK11/CDK19 Inhibitor, CDK8 Inhibitor, cFMS Inhibitor V, CSF-1 Receptor Inhibitor V, CSF1R Inhibitor V, DDR2 Inhibitor II, Flt-3 Inhibitor VIII, IL-34 Receptor Inhibitor V, NTRK3/TrkC Inhibitor, VEGFR Tyrosine Kinase Inhibitor XXXVI, VEGFR2 Tyrosine Kinase Inhibitor XXXIV, PLX-647, c-Kit Inhibitor IV) 10mg　217366

特徴

• A cell-permeable and bio-available azaindolylmethylpyridamine derivative that acts as a potent inhibitor against FMS and KIT (IC50 = 28 and 16nM, 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 710nM, respectively) and exhibiting much reduced or little potency toward other kinases in a 400-kinase panel study (IC50 >1uM). Shown to effectively inhibit cellular FLT3-ITD, FMS, KIT phosphorylations (IC50 from 20 to 250nM), as well as FLT3-ITD-, FMS-, KIT-dependent proliferations (IC50 from 92 to 380nM). Exhibits in vivo efficacy in several murine inflammation models (20 to 80mg/kg b.i.d.; p.o.) and in preventing rat MRMT-1 breast carcinoma bone metastases-caused osteolysis (30mg/kg b.i.d.; p.o.).
• Alternate Names:PLX-647, c-Kit Inhibitor IV, CDC2L6/CDK11/CDK19 Inhibitor, CDK8 Inhibitor, cFMS Inhibitor V, CSF-1 Receptor Inhibitor V, CSF1R Inhibitor V, DDR2 Inhibitor II, Flt-3 Inhibitor VIII, IL-34 Receptor Inhibitor V, NTRK3/TrkC Inhibitor, VEGFR Tyrosine Kinase Inhibitor XXXVI, VEGFR2 Tyrosine Kinase Inhibitor XXXIV
• Molecular Formula:C₂₁H₁₇F₃N₄
• Form:Supplied as an off-white powder.
• Solubility:DMSO
• Primary Target:FMS
• Secondary Target:KIT
• Storage and Stability:Store at -20°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.