中文名 | PCI 29732 |
英文名 | PCI 29732 |
别名 | 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 |
英文别名 | CS-2698 PCI29732 PCI-29732 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)- |
CAS | 330786-25-9 |
化学式 | C22H21N5O |
分子量 | 371.43 |
密度 | 1.36±0.1 g/cm3(Predicted) |
沸点 | 599.6±50.0 °C(Predicted) |
溶解度 | DMSO : ≥ 53 mg/mL (142.69 mM) 乙醇: 10 mg/mL (26.92 mM; 需超声) |
酸度系数 | 4.24±0.30(Predicted) |
存储条件 | -20℃ |
体外研究 | PCI29732 shows cytotoxicity in different cells. The IC 50 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). |
体内研究 | 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. Animal Model: 5-6 weeks old athymic nude mice (bearing H460/MX20 cells) Dosage: 20 mg/kg (combination with Topotecan; every 3 d × 5 times, i.p., 3 mg/kg; topotecan was given 1 h after PCI29732 administration) Administration: P.o.; every 3 d × 5 times Result: Significant reductions in tumor weight and volume were observed in the group treated with PCI29732 in combination with Topotecan. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.692 ml | 13.461 ml | 26.923 ml |
5 mM | 0.538 ml | 2.692 ml | 5.385 ml |
10 mM | 0.269 ml | 1.346 ml | 2.692 ml |
5 mM | 0.054 ml | 0.269 ml | 0.538 ml |
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