PLX647
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- Product name: PLX647
- CAS: 873786-09-5
- MF: C21H17F3N4
- MW: 382.38
- EINECS:
- MDL Number:MFCD28100808
- Synonyms:PLX647;PLC647;5-(1H-Pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-2-pyridinamine;[5-[(1H-Pyrrolo[2,3-b]pyridin-3-yl)methyl]pyridin-2-yl](4-trifluoromethylbenzyl)amine;2-Pyridinamine, 5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-;PLX 647;PLX-647;CS-1696;5-({1H-pyrrolo[2,3-b]pyridin-3-yl}methyl)-N-{[4-(trifluoromethyl)phenyl]methyl}pyridin-2-amine
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Properties
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
storage temp. :2-8°C
solubility :DMSO: soluble20mg/mL, clear
form :powder
pka :13.73±0.40(Predicted)
color :white to beige
Safety Information
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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.Suppliers and manufacturers
ATK CHEMICAL COMPANY LIMITED
BOC Sciences
TargetMol Chemicals Inc.
Zhejiang J&C Biological Technology Co.,Limited
InvivoChem
ShenZhen Trendseen Biological Technology Co.,Ltd.
Wuhan Topule Biopharmaceutical Co., Ltd
Zibo Hangyu Biotechnology Development Co., Ltd
Amadis Chemical Company Limited
Angel Pharmatech, Ltd.