基本属性 生物活性体外研究体内研究 用途与合成方法 10MG 价格(试剂级) 供应商 供应信息 相关产品
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10MG

10MG

中文名称:10MG
英文名称:PLX647
CAS号:873786-09-5
分子式:C21H17F3N4
分子量:382.38
EINECS号:
Mol文件:873786-09-5.mol
10MG 结构式

10MG 性质

密度 1.358±0.06 g/cm3(Predicted)
储存条件 2-8°C
溶解度 在DMSO中的溶解度为20mg/mL,澄清
形态 粉末
酸度系数(pKa) 13.73±0.40(Predicted)
颜色 白色至米色

10MG 用途与合成方法

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)。

In vitro, PLX647 potently inhibits proliferation of BCR-FMS cells, with an IC 50 of 92 nM. A corresponding Ba/F3 cell line expressing BCR-KIT is also quite sensitive to PLX647, with an IC 50 of 180 nM. PLX647 also inhibits endogenous FMS and KIT, as demonstrated by inhibition of the ligand-dependent cell lines M-NFS-60 (IC 50 =380 nM) and M-07e (IC 50 =230 nM), which express FMS and KIT, respectively.
PLX647 potently inhibits the growth of FLT3–ITD-expressing MV4-11 cells (IC 50 =110 nM). PLX647 displayed minimal inhibition of the proliferation of Ba/F3 cells expressing BCR–KDR (IC 50 =5 μM). PLX647 inhibits osteoclast differentiation with an IC 50 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.

安全信息

危险品标志Xi
危险类别码36/37/38
安全说明36/37/39
WGK Germany3

10MG 价格(试剂级)

更新日期 产品编号 产品名称 CAS号 包装 价格
2024-01-25 HY-13838 873786-09-5 5mg 600
2024-01-25 HY-13838 873786-09-5 10mM * 1mLin DMSO 660

10MG供应商 更多

上海楼岚生物科技有限公司
联系电话:021-52996696,15000506266 15000506266
产品介绍:
英文名称:PLX647
CAS:873786-09-5
包装信息:MG,G
备注:标准品
广州致雅医药科技有限公司
联系电话: 18122150900
产品介绍:
英文名称:PLX647
CAS:873786-09-5
纯度:99%
上海一飞生物科技有限公司
联系电话:021-65675885 18964387627
产品介绍:
英文名称:PLX647
CAS:873786-09-5
纯度:95%
包装信息:5mg;10mg;25mg
备注:试剂级
上海瀚香生物科技有限公司
联系电话:17754423994 17754423994
产品介绍:
英文名称:PLX647
CAS:873786-09-5
纯度:98% HPLC LCMS
包装信息:100mg;1g
备注:量大优惠,现货促销
滁州市科迈尔化工科技有限公司
联系电话:0550-5196001 15000891977
产品介绍:
英文名称:PLX647
CAS:873786-09-5
纯度:98%HPLC
包装信息:1mg,10mg,100mg,500mg,1g,10g

最新发布供应信息

FMS/KIT双重抑制剂(PLX647)
上海泽叶生物科技有限公司 2024-04-26

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