873786-09-5
基本信息
PLX647
CS-1696
PLX 647
PLX-647
[5-[(1H-Pyrrolo[2,3-b]pyridin-3-yl)methyl]pyridin-2-yl](4-trifluoromethylbenzyl)amine
5-(1H-Pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-2-pyridinamine
2-Pyridinamine, 5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-
物理化学性质
| 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 |
| 颜色 | 白色至米色 |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H319-H315-H335 |
| 防范说明 | P264-P280-P305+P351+P338-P337+P313P-P264-P280-P302+P352-P321-P332+P313-P362 |
| 危险品标志 | Xi |
| 危险类别码 | 36/37/38 |
| 安全说明 | 36/37/39 |
| WGK Germany | 3 |
10MG价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/04/30 | HY-13838 | PLX647 | 873786-09-5 | 5mg | 600元 |
| 2024/04/30 | HY-13838 | PLX647 | 873786-09-5 | 10mM * 1mLin DMSO | 660元 |
| 2024/04/30 | HY-13838 | PLX647 | 873786-09-5 | 10mg | 900元 |
常见问题列表
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. |