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PLX647

CAS No. : 873786-09-5

MCE 国际站：PLX647

产品活性：PLX647 是一种高度特异性的，具有口服活性的 FMS 和 KIT 双激酶抑制剂，IC₅₀ 分别为 28 和 16 nM。PLX647 (1 μM) 在 400 个激酶组中显示出对 FMS 和 KIT 有选择性，但 FLT3 和 KDR 除外 (IC₅₀=91 和 130 nM)。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：c-Fms  |  c-Kit

In Vitro: In vitro, PLX647 potently inhibits proliferation of BCR-FMS cells, with an IC₅₀ of 92 nM. A corresponding Ba/F3 cell line expressing BCR-KIT is also quite sensitive to PLX647, with an IC₅₀ of 180 nM. PLX647 also inhibits endogenous FMS and KIT, as demonstrated by inhibition of the ligand-dependent cell lines M-NFS-60 (IC₅₀=380 nM) and M-07e (IC₅₀=230 nM), which express FMS and KIT, respectively.
PLX647 potently inhibits the growth of FLT3–ITD-expressing MV4-11 cells (IC₅₀=110 nM). PLX647 displayed minimal inhibition of the proliferation of Ba/F3 cells expressing BCR–KDR (IC₅₀=5 μM). PLX647 inhibits osteoclast differentiation with an IC₅₀ of 0.17 μM.

In Vivo: PLX647 (40 mg/kg; p.o.; twice daily for 7 days) reduces macrophage accumulation in UUO kidney and blood monocytes.
PLX647 (40 mg/kg; p.o.; male Swiss Webster mice) reduces LPS-induced TNF-α and IL-6 release.
PLX647 (20-80 mg/kg; p.o.; daily or twice daily from 27-41 days) shows effects on collagen-induced arthritis.
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.

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