330786-25-9
基本信息
4-氨基-1-環(huán)戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶
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)-
物理化學性質
報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
2024/11/08 | HY-18010 | 4-氨基-1-環(huán)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 |
2024/11/08 | HY-18010 | 4-氨基-1-環(huán)戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶 PCI 29732 | 330786-25-9 | 10mM * 1mLin DMSO | 1100元 |
2024/11/08 | HY-18010 | 4-氨基-1-環(huán)戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶 PCI 29732 | 330786-25-9 | 10mg | 1600元 |
常見問題列表
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. |