网站主页 >> CAS数据库列表 >> N-[5-[2-AMINO-7-(1-HYDROXY-2-METHYLPROPAN-2-YL)PYRROLO[2,3-D]PYRIMIDINE-5-CARBONYL]PYRIDIN-3-YL]-2-(5-CHLOROPYRIDIN-2-YL)ACETAMIDE
N-[5-[2-AMINO-7-(1-HYDROXY-2-METHYLPROPAN-2-YL)PYRROLO[2,3-D]PYRIMIDINE-5-CARBONYL]PYRIDIN-3-YL]-2-(5-CHLOROPYRIDIN-2-YL)ACETAMIDE
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- CAS号:
- 1402438-74-7
- 英文名:
- PF-06273340
- 英文别名:
- PF6273340;PF-6273340;PF 6273340;PF-06273340;PF-06273340 >=98% (HPLC);BPIWZDNVMQQBQX-UHFFFAOYSA-N;inhibit,Trk Receptor,PF-06273340,PF06273340,Tropomyosin related kinase receptor,Inhibitor;N-[5-[[2-Amino-7-(2-hydroxy-1,1-dimethylethyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]carbonyl]-3-pyridinyl]-5-chloro-2-pyridineacetamide;N-[5-[2-AMINO-7-(1-HYDROXY-2-METHYLPROPAN-2-YL)PYRROLO[2,3-D]PYRIMIDINE-5-CARBONYL]PYRIDIN-3-YL]-2-(5-CHLOROPYRIDIN-2-YL)ACETAMIDE;2-Pyridineacetamide, N-[5-[[2-amino-7-(2-hydroxy-1,1-dimethylethyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]carbonyl]-3-pyridinyl]-5-chloro-
- 中文名:
- N-[5-[2-AMINO-7-(1-HYDROXY-2-METHYLPROPAN-2-YL)PYRROLO[2,3-D]PYRIMIDINE-5-CARBONYL]PYRIDIN-3-YL]-2-(5-CHLOROPYRIDIN-2-YL)ACETAMIDE
- 中文别名:
- 化合物PF-06273340
- CBNumber:
- CB93165808
- 分子式:
- C23H22ClN7O3
- 分子量:
- 479.92
- MOL File:
- 1402438-74-7.mol
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N-[5-[2-AMINO-7-(1-HYDROXY-2-METHYLPROPAN-2-YL)PYRROLO[2,3-D]PYRIMIDINE-5-CARBONYL]PYRIDIN-3-YL]-2-(5-CHLOROPYRIDIN-2-YL)ACETAMIDE化学性质
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密度:
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1.47±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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12.40±0.70(Predicted)
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N-[5-[2-AMINO-7-(1-HYDROXY-2-METHYLPROPAN-2-YL)PYRROLO[2,3-D]PYRIMIDINE-5-CARBONYL]PYRIDIN-3-YL]-2-(5-CHLOROPYRIDIN-2-YL)ACETAMIDE性质、用途与生产工艺
PF-06273340是一种高度有效的、具有激酶选择性的、耐受良好的泛Trk抑制剂,对TrkA、TrkB、TrkC的IC50值分别为6 nM、4 nM、3 nM。
Target | Value |
TrkC
(Cell-free assay)
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3 nM
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TrkB
(Cell-free assay)
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4 nM
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TrkA
(Cell-free assay)
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6 nM
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PF-06273340是一种高度有效的泛Trk抑制剂,具有良好的亲脂性。PF-06273340在各种体外安全性试验中进行测试,在THLE或HepG2细胞系中有微小的毒性作用(IC50分别大于42 μM和300 μM)。在激酶选择性实验中,所有的IC50/Ki值大于10 μM,除了COX1(IC50=2.7 μM)、多巴胺转运体实验(Ki=5.2 μM)和PDEs 4D, 5A, 7B, 8B和11(在PF-06273340浓度为10 μM时,达到54%-89%的抑制率)。在309种激酶试验中,只有不到40%的激酶被1 μM PF-06273340抑制,除了MUSK(IC50=53 nM)、FLT-3(IC50=395 nM)、IRAK1(IC50=2.5 μM), MKK(1 μM浓度时抑制率为90%)和DDR1(1 μM浓度时抑制率为60%)。
在大鼠中,给药浓度为150 mg/kg/d时,体内白细胞数量减少;而当剂量≥250 mg/kg时候,体增重和摄食量增加,这可能是由于抑制了TrkB所引起,TrkB的激动剂可在啮齿类动物中引起厌食反应。通过显微镜观察,肝脏也发生了适应性改变,剂量≥250 mg/kg时,肝脏重量增加;剂量为1000 mg/kg时,胆固醇增加。浓度高达1000 mg/kg/天时,PF-06273340依然耐受良好,此时血浆中药物浓度将近是对TrkA IC50的400倍。
N-[5-[2-AMINO-7-(1-HYDROXY-2-METHYLPROPAN-2-YL)PYRROLO[2,3-D]PYRIMIDINE-5-CARBONYL]PYRIDIN-3-YL]-2-(5-CHLOROPYRIDIN-2-YL)ACETAMIDE
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 |
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2024/04/30 | S8407 | N-[5-[2-AMINO-7-(1-HYDROXY-2-METHYLPROPAN-2-YL)PYRROLO[2,3-D]PYRIMIDINE-5-CARBONYL]PYRIDIN-3-YL]-2-(5-CHLOROPYRIDIN-2-YL)ACETAMIDE PF-06273340 | 1402438-74-7 | 10mg | 1040.15元 |
2024/04/30 | HY-122616 | PF-06273340 | | 1 mg | 1200元 |
N-[5-[2-AMINO-7-(1-HYDROXY-2-METHYLPROPAN-2-YL)PYRROLO[2,3-D]PYRIMIDINE-5-CARBONYL]PYRIDIN-3-YL]-2-(5-CHLOROPYRIDIN-2-YL)ACETAMIDE
生产厂家
1402438-74-7, N-[5-[2-AMINO-7-(1-HYDROXY-2-METHYLPROPAN-2-YL)PYRROLO[2,3-D]PYRIMIDINE-5-CARBONYL]PYRIDIN-3-YL]-2-(5-CHLOROPYRIDIN-2-YL)ACETAMIDE 相关搜索:
- 科研试剂
- 化合物PF-06273340
- 1402438-74-7
- inhibit,Trk Receptor,PF-06273340,PF06273340,Tropomyosin related kinase receptor,Inhibitor
- PF-6273340
- PF6273340
- PF 6273340
- PF-06273340 >=98% (HPLC)
- 2-Pyridineacetamide, N-[5-[[2-amino-7-(2-hydroxy-1,1-dimethylethyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]carbonyl]-3-pyridinyl]-5-chloro-
- N-(5-(2-amino-7-(1-hydroxy-2-methylpropan-2-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonyl)pyridin-3-yl)-2-(5-chloropyridin-2-yl)acetamide
- N-[5-[[2-Amino-7-(2-hydroxy-1,1-dimethylethyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]carbonyl]-3-pyridinyl]-5-chloro-2-pyridineacetamide
- BPIWZDNVMQQBQX-UHFFFAOYSA-N
- N-[5-[2-AMINO-7-(1-HYDROXY-2-METHYLPROPAN-2-YL)PYRROLO[2,3-D]PYRIMIDINE-5-CARBONYL]PYRIDIN-3-YL]-2-(5-CHLOROPYRIDIN-2-YL)ACETAMIDE
- PF-06273340