4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶
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- CAS号:
- 330786-25-9
- 英文名:
- PCI 29732
- 英文别名:
- CS-2698;PCI 29732;PCI 29732;PCI29732;PCI-29732;PCI 29732 (This product is only available in Japan.);1-Cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine;4-Amino-1-cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine;1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 1-cyclopentyl-3-(4-phenoxyphenyl)-;cytotoxicity,Bruton tyrosine kinase,Inhibitor,Btk,ABCG2,reversible,PCI 29732,BCR,inhibit,B-cell,BCRP,oral,Breast cancer resistance protein
- 中文名:
- 4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶
- 中文别名:
- 化合物PCI29732;PCI 29732,BTK抑制剂;4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶
- CBNumber:
- CB12668434
- 分子式:
- C22H21N5O
- 分子量:
- 371.43
- MOL File:
- 330786-25-9.mol
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4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶化学性质
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沸点:
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599.6±50.0 °C(Predicted)
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密度:
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1.36±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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DMF: 20 mg/ml; DMF:PBS (pH 7.2) (1:2): 0.3 mg/ml; DMSO: 10 mg/ml; Ethanol: 5 mg/ml
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酸度系数(pKa):
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4.24±0.30(Predicted)
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形态:
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Powder
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4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶性质、用途与生产工艺
PCI 29732是一种选择性的、不可逆的Btk抑制剂，IC50为0.5 nM。
| Target | Value |
BTK
(Cell-free assay)
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0.5 nM
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BLK
(Cell-free assay)
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0.5 nM
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Bmx
(Cell-free assay)
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0.8 nM
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EGFR
(Cell-free assay)
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5.6 nM
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YES
(Cell-free assay)
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6.5 nM
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PCI29732 shows cytotoxicity in different cells. The IC
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values are 7.94 μM for S1, 7.79 μM for S1-MI-80, 6.55 μM for H460, 6.34 μM for H460/MX20, 6.14 μM for KB, 6.02 μM for KBv200, 12.45 μM for HEK293/pcDNA3, 14.58 μM for HEK293-ABCG2-482-R2, and 13.24 μM for HEK293-ABCG2-482-T7 cells.
PCI-29732 blocks the transcriptional up-regulation of a panel of B-cell activation genes in human CD20+ B cells stimulated at the B-cell antigen receptor (BCR).
PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 and enhances the anti-tumor efficacy of substrate chemotherapeutic agents.
PCI 29732 (20 mg/kg; p.o.; every 3 d × 5 times) enhances the anticancer efficacy of Topotecan in the H460/MX20 cell xenograft nude mice model.
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Animal Model:
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5-6 weeks old athymic nude mice (bearing H460/MX20 cells)
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Dosage:
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20 mg/kg (combination with Topotecan; every 3 d × 5 times, i.p., 3 mg/kg; topotecan was given 1 h after PCI29732 administration)
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Administration:
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P.o.; every 3 d × 5 times
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Result:
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Significant reductions in tumor weight and volume were observed in the group treated with PCI29732 in combination with Topotecan.
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4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶
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 |
|---|
| 2024/04/30 | HY-18010 | 4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶
PCI 29732 | 330786-25-9 | 5mg | 1000元 |
| 2024/04/30 | S6725 | 4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶
PCI 29732 | 330786-25-9 | 2mg | 1050.21元 |
4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶
生产厂家
330786-25-9, 4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶 相关搜索:
- 药靶配体
- PCI 29732,BTK抑制剂
- 化合物PCI29732
- 4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶
- 330786-25-9
- cytotoxicity,Bruton tyrosine kinase,Inhibitor,Btk,ABCG2,reversible,PCI 29732,BCR,inhibit,B-cell,BCRP,oral,Breast cancer resistance protein
- 1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 1-cyclopentyl-3-(4-phenoxyphenyl)-
- PCI 29732;PCI29732;PCI-29732
- CS-2698
- PCI 29732 (This product is only available in Japan.)
- 1-Cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
- 4-Amino-1-cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine
- PCI 29732