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

Safety

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

36/37/39

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

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.

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.