10MG
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- CAS号:
- 873786-09-5
- 英文名:
- PLX647
- 英文别名:
- PLC647;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]-
- 中文名:
- 10MG
- 中文别名:
- 化合物PLX647;FMS/KIT双重抑制剂(PLX647)
- CBNumber:
- CB72667277
- 分子式:
- C21H17F3N4
- 分子量:
- 382.38
- MOL File:
- 873786-09-5.mol
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10MG化学性质
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密度:
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1.358±0.06 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO: soluble20mg/mL, clear
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形态:
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powder
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酸度系数(pKa):
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13.73±0.40(Predicted)
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颜色:
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white to beige
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10MG性质、用途与生产工艺
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.
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Animal Model:
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Male C57BL/6 mice (mouse unilateral ureter obstruction model)
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Dosage:
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40 mg/kg
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Administration:
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P.o.; twice daily for 7 days
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Result:
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Resulted in reduction in the levels of F4/80+ macrophages by 77%.
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Animal Model:
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7-9 wk old Male DBA/1J mice (Mouse collagen-induced arthritis model)
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Dosage:
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20 mg/kg, 80 mg/kg
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Administration:
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P.o.; daily (20 mg/kg) from 27-41 days, twice daily (80 mg/kg) from 27-41 days
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Result:
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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.
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10MG
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-13838 | PLX647 | 873786-09-5 | 5mg | 600元 |
| 2024/01/25 | HY-13838 | PLX647 | 873786-09-5 | 10mM * 1mLin DMSO | 660元 |
10MG
生产厂家
全球有 58家供应商
10MG国内生产厂家
873786-09-5, 10MG 相关搜索:
- Inhibitors
- 细胞生物学试剂
- 小分子抑制剂，天然产物
- 小分子抑制剂
- C21H17F3N4
- 化合物PLX647
- FMS/KIT双重抑制剂(PLX647)
- 873786-09-5
- CS-1696
- PLX 647;PLX-647
- 2-Pyridinamine, 5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-
- [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
- PLC647
- PLX647