| 中文名称: | PLX647 | ||||
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| 英文名称: | PLX647 | ||||
| 别名: | PLX647 5-(1h-Pyrrolo[2,3-B]pyridin-3-Ylmethyl)-N-[4-(Trifluoromethyl)benzyl]pyridin-2-Amine | ||||
| CAS No: | 873786-09-5 | 分子式: | C21H17F3N4 | 分子量: | 382.38 |
| CAS No: | 873786-09-5 | ||||
| 分子式: | C21H17F3N4 | ||||
| 分子量: | 382.38 | ||||
基本信息
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产品编号：P70161 |
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产品名称：PLX647 |
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CAS: |
873786-09-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
382.38 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
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Ethanol |
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Water |
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体内（现配现用） |
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＜1mg/ml表示微溶或不溶。 |
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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。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.6152mL |
13.0760mL |
26.1520mL |
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5mM |
0.5230mL |
2.6152mL |
5.2304mL |
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10mM |
0.2615mL |
1.3076mL |
2.6152mL |
生物活性
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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)。 |
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靶点/IC50 |
c-Fms |
c-Kit |
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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. |
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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. |
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Animal Model: |
Male C57BL/6mice (mouse unilateral ureter obstruction model |
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Dosage: |
40mg/kg |
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Administration: |
P.o.;twice daily for 7days |
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Result: |
Resulted in reduction in the levels of F4/80+ macrophages by 77% |
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Animal Model: |
7-9 wk old Male DBA/1J mice (Mouse collagen-induced arthritis model) |
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Dosage: |
20mg/kg, 80mg/kg |
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Administration: |
P.o;daily (20mg/kg) from 27-41days, twice daily (80mg/kg) from 27-41days |
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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. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
