PLX647  ≥98%

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包装规格:5mg 10mg 50mg 100mg in glass bottle
溶解性:溶于DMSO(25mg/mL超声)
产品描述:基本信息 产品编号:P70161 产品名称:PLX647 CAS: 873786-09-5   储存条件 粉末 -20℃ 四年     分子式: C21H17F3N4 溶于液体 -80℃ 六个月 分子量 382.38 -20℃ 一个月 化学名:      Solubility (25°C)   体外 DMSO   Ethanol   Water   体内(现配现用)     <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.6152mL 13.0760mL 26.1520mL 5mM 0.5230mL 2.6152mL 5.2304mL 10mM 0.2615mL 1.3076mL 2.6152mL   生物活性 产品描述 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 16nM。PLX647 (1μM) 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 130nM)。 靶点/IC50 c-Fms c-Kit   体外研究 In vitro, PLX647 potently inhibits proliferation of BCR-FMS cells, with an IC50 of 92nM. A corresponding Ba/F3 cell line expressing BCR-KIT is also quite sensitive to PLX647, with an IC50 of 180nM. PLX647 also inhibits endogenous FMS and KIT,as demonstrated by inhibition of the ligand-dependent cell lines M-NFS-60 (IC50=380nM) and M-07e (IC50=230nM), which express FMS and KIT, respectively. PLX647 potently inhibits the growth of FLT3–ITD-expressing MV4-11 cells (IC50=110nM). PLX647 displayed minimal inhibition of the proliferation of Ba/F3 cells expressing BCR–KDR (IC50=5μM). PLX647 inhibits osteoclast differentiation with an IC50 of 0.17μM.   体内研究 PLX647 (40mg/kg; p.o; twice daily for 7days) reduces macrophage accumulation in UUO kidney and blood monocytes.PLX647 (40mg/kg; p.o.; male Swiss Webster mice) reduces LPS-induced TNF-αand IL-6 release.PLX647 (20-80mg/kg; p.o.; daily or twice daily from 27-41days) shows effects on collagen-induced arthritis.PLX647 (30mg/kg) results in significant inhibition of TRAP5b immunostaining and bone osteolysis. PLX647 (30mg/kg BID) is able to prevent bone damage by the tumor cells. Animal Model: Male C57BL/6mice (mouse unilateral ureter obstruction model Dosage: 40mg/kg Administration: P.o.;twice daily for 7days 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: 20mg/kg, 80mg/kg Administration: P.o;daily (20mg/kg) from 27-41days, twice daily (80mg/kg) from 27-41days Result: 20mg/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 80mg/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.
保存条件:-20℃