PLX647

SKU: orb1223776

Description

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

Key Properties

• CAS Number: 873786-09-5
• MW: 382.38
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₇F₃N₄
• SMILES: FC(C1=CC=C(C=C1)CNC2=NC=C(CC3=CNC4=NC=CC=C43)C=C2)(F)F
• Target: CSF1R
• Solubility: DMSO: 20 mg/mL

Bioactivity

• 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. 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PLX647 | PLX 647 | PLX-647.

Quick Database Links

Gene Symbol

CSF1R