4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶
4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶
![4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶 结构式](https://img.chemicalbook.com/CAS/20150408/GIF/330786-25-9.gif)
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
| 沸点 | 599.6±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.36±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMF：20mg/mL； DMF:PBS (pH 7.2) (1:2)：0.3 mg/mL； DMSO：10mg/mL；乙醇：5mg/mL |
| 酸度系数(pKa) | 4.24±0.30(Predicted) |
| 形态 | 粉末 |
4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶 用途与合成方法
| Target | Value |
|
BTK
(Cell-free assay) | 0.5 nM |
|
BLK
(Cell-free assay) | 0.5 nM |
|
Bmx
(Cell-free assay) | 0.8 nM |
|
EGFR
(Cell-free assay) | 5.6 nM |
|
YES
(Cell-free assay) | 6.5 nM |
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).
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. |
4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-01-25 | 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 | 330786-25-9 | 5mg | 1000 |
| 2024-01-25 | 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 | 330786-25-9 | 10mM * 1mLin DMSO | 1100 |
