ChemicalBook > CAS DataBase List > PLX647

PLX647

PLX647 Structure
PLX647
  • CAS No.873786-09-5
  • Chemical Name:PLX647
  • CBNumber:CB72667277
  • Molecular Formula:C21H17F3N4
  • Formula Weight:382.38
  • MOL File:873786-09-5.mol
PLX647 Property
  • Density 1.358±0.06 g/cm3(Predicted)
  • storage temp. 2-8°C
  • solubility DMSO: soluble20mg/mL, clear
  • form powder
  • pka 13.73±0.40(Predicted)
  • color white to beige
  • UNSPSC Code 12352200
Safety
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H319-H315-H335
  • Precautionary statements P264-P280-P305+P351+P338-P337+P313P-P264-P280-P302+P352-P321-P332+P313-P362

PLX647 Chemical Properties,Usage,Production

  • Description PLX647 is a dual inhibitor of the receptor tyrosine kinases FMS and KIT (IC50s = 28 and 16 nM, respectively). It is selective for FMS and KIT but does inhibit FLT3 and KDR (IC50s = 91 and 130 nM, respectively) in a panel of 400 kinases at a concentration of 1 μM. PLX647 inhibits proliferation of Ba/F3 cells expressing constitutively active FMS or KIT (IC50s = 92 and 180 nM, respectively) as well as ligand-dependent growth of M-NFS-60 and M-07e cells that express endogenous FMS and KIT, respectively (IC50s = 380 and 230 nM, respectively). It has no effect on HEK293T or HepG2 cells that lack FMS and KIT (IC50 = >50 μM) or Ba/F3 cells overexpressing KDR (IC50 = >5 μM). PLX647 also inhibits differentiation of human osteoclast precursor cells (IC50 = 170 nM). In vivo, PLX647 (40 mg/kg) reduces TNF-α and IL-6 release in a rat model of LPS-induced cytokine release. It reduces mast cell degranulation in a mouse model of passive cutaneous anaphylaxis (PCA) and inhibits bone destruction and delays disease progression in a mouse model of collagen-induced arthritis (CIA). PLX647 also reverses bone osteolysis and allodynia in a syngeneic rat model of cancer-induced bone pain.
  • Uses PLX647 is a novel tyrosine kinase (TK) inhibitor, which selectively targets c-Kit and c-Fms.
  • in vivo

    PLX647 (40 mg/kg; p.o.; twice daily for 7 days) reduces macrophage accumulation in UUO kidney and blood monocytes[1].
    PLX647 (40 mg/kg; p.o.; male Swiss Webster mice) reduces LPS-induced TNF-α and IL-6 release[1].
    PLX647 (20-80 mg/kg; p.o.; daily or twice daily from 27-41 days) shows effects on collagen-induced arthritis[1].
    PLX647 (30 mg/kg) results in significant inhibition of TRAP5b immunostaining and bone osteolysis. PLX647 (30 mg/kg BID) is able to prevent bone damage by the tumor cells[1].

    Animal Model:Male C57BL/6 mice (mouse unilateral ureter obstruction model)[1]
    Dosage:40 mg/kg
    Administration:P.o.; twice daily for 7 days
    Result:Resulted in reduction in the levels of F4/80+ macrophages by 77%.
    Animal Model:7-9 wk old Male DBA/1J mice (Mouse collagen-induced arthritis model)[1]
    Dosage:20 mg/kg, 80 mg/kg
    Administration:P.o.; daily (20 mg/kg) from 27-41 days, twice daily (80 mg/kg) from 27-41 days
    Result:20 mg/kg PLX647 had no initial effect on the development of severe arthritis. However, starting on day 33, no further development of disease severity was recorded, and a 30% inhibition of the macroscopic signs of arthritis was evident in clinical score on day 41. Mice treated with 80 mg/kg BID PLX647 initially shows delayed development of severe arthritic signs. Starting on day 33, the signs of arthritis began to decrease in this treatment group, reaching a maximum reversal of 76% on day 41.
  • References [1]. zhang c, ibrahim pn, zhang j, et al. design and pharmacology of a highly specific dual fms and kit kinase inhibitor. proc natl acad sci u s a, 2013, 110(14): 5689-5694.
PLX647 Preparation Products And Raw materials
Raw materials
Preparation Products
PLX647 Suppliers
Global(68)Suppliers
  • Supplier：
    BOC Sciences
  • Tel：+1-631-485-4226
  • Email：inquiry@bocsci.com
  • Country：United States
  • ProdList：19552
  • Advantage：58
  • Supplier：
    TopScience Biochemical
  • Tel：00852-68527855
  • Email：info@itopbiochem.com
  • Country：China Hong Kong
  • ProdList：902
  • Advantage：58
  • Supplier：
    TargetMol Chemicals Inc.
  • Tel：+1-781-999-5354<br/>+1-00000000000
  • Email：marketing@targetmol.com
  • Country：United States
  • ProdList：32159
  • Advantage：58
  • Supplier：
    InvivoChem
  • Tel：+1-708-310-1919<br/>+1-13798911105
  • Email：sales@invivochem.cn
  • Country：United States
  • ProdList：6391
  • Advantage：58
  • Supplier：
    TargetMol Chemicals Inc.
  • Tel：
  • Email：support@targetmol.com
  • Country：United States
  • ProdList：38630
  • Advantage：58
PLX647 Spectrum
873786-09-5, PLX647Related Search:
  • Inhibitors
  • 抑制剂
  • 细胞生物学试剂
  • 小分子抑制剂，天然产物
  • 小分子抑制剂
  • C21H17F3N4
  • 化合物PLX647
  • FMS/KIT双重抑制剂(PLX647)
  • 873786-09-5
  • FMS/KIT Dual Kinase Inhibitor, PLX647
  • 5-({1H-pyrrolo[2,3-b]pyridin-3-yl}methyl)-N-{[4-(trifluoromethyl)phenyl]methyl}pyridin-2-amine
  • CS-1696
  • PLX 647;PLX-647
  • 2-Pyridinamine, 5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-
  • [5-[(1H-Pyrrolo[2,3-b]pyridin-3-yl)methyl]pyridin-2-yl](4-trifluoromethylbenzyl)amine
  • 5-(1H-Pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-2-pyridinamine
  • PLC647
  • PLX647

Home

My