PLX647

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PLX647 是一种高度特异性的双 FMS/KIT 激酶抑制剂，IC50 分别为 28/16 nM。

PLX647 is a highly specific dual FMS/KIT kinase inhibitor with IC50 of 28/16 nM respectively.

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.

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. Animal Model:Male C57BL/6 mice (mouse unilateral ureter obstruction model)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) 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.

PLX647 | PLX 647 | PLX-647.

Tyrosine Kinase

CSF1R

c-Fms| c-Kit

Cancer

——

873786-09-5

382.38

C21H17F3N4

>98% (HPLC)

DMSO: 20 mg/mL

FC(C1=CC=C(C=C1)CNC2=NC=C(CC3=CNC4=NC=CC=C43)C=C2)(F)F

5-((1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)-N-(4-(trifluoromethyl)benzyl)pyridin-2-amine

(-20℃)

With Ice Pack

≥ 2 years