PLX647 dihydrochloride Biochemical | PLX647 biochemical

PLX647 dihydrochloride

Cat. Num. AAA227893

• Purity: 98%
• Synonyms: PLX647 dihydrochloride; N/A; PLX647 biochemical

• Purity/Purification: 98%

• CAS: 1779796-38-1
• Solubility: <1mg/ml refers to the product slightly soluble or insoluble
• In vitro: PLX647 dihydrochloride (40 mg/kg; p.o.; twice daily for 7 days) reduces macrophage accumulation in UUO kidney and blood monocytes[1]. PLX647 dihydrochloride (40 mg/kg; p.o.; male Swiss Webster mice) reduces LPS-induced TNF-alpha and IL-6 release[1]. PLX647 dihydrochloride (20-80 mg/kg; p.o.; daily or twice daily from 27-41 days) shows effects on collagen-induced arthritis[1]. PLX647 dihydrochloride (30 mg/kg) results in significant inhibition of TRAP5b immunostaining and bone osteolysis. PLX647 dihydrochloride (30 mg/kg BID) is able to prevent bone damage by the tumor cells[1]. Animal Model: Male C57BL/6 mice (mouse unilateral ureter obstruction model)[1]. 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)[1]. 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.
• Preparation and Storage: Powder: -20 degree C for 3 years; In solvent: -80 degree C for 2 years

Structure

(Ac-Ile-Glu-Thr-Asp-pNA, CAS 219138-21-3)

Structure

(Ac-Ile-Glu-Thr-Asp-pNA, CAS 219138-21-3)

Related Product Information for PLX647 biochemical

PLX647 dihydrochloride is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC 50 s of 28 and 16 nM, reapectively. PLX647 dihydrochloride shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 uM except FLT3 and KDR (IC 50 s=91 and 130 nM, respectively).

References

1. Smith GK, et al. Expression, preparation, and high-throughput screening of caspase-8: discovery of redox-based and steroid diacid inhibition. Arch Biochem Biophys. 2002;399(2):195-205.