Chemical Property of 5-(1h-Pyrrolo[2,3-B]pyridin-3-Ylmethyl)-N-[4-(Trifluoromethyl)benzyl]pyridin-2-Amine
Chemical Property:
- Storage Temp.:2-8°C
- Solubility.:DMSO: soluble20mg/mL, clear
- XLogP3:4.9
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:6
- Rotatable Bond Count:5
- Exact Mass:382.14053105
- Heavy Atom Count:28
- Complexity:493
- Purity/Quality:
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99%, *data from raw suppliers
PLX647 *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:Xi
- Statements:
36/37/38
- Safety Statements:
36/37/39
- MSDS Files:
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Useful:
- Canonical SMILES:C1=CC2=C(NC=C2CC3=CN=C(C=C3)NCC4=CC=C(C=C4)C(F)(F)F)N=C1
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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.
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Uses
PLX647 is a novel tyrosine kinase (TK) inhibitor, which selectively targets c-Kit and c-Fms.
