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330786-25-9

中文名稱 4-氨基-1-環(huán)戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶
英文名稱 PCI 29732
CAS 330786-25-9
分子式 C22H21N5O
分子量 371.43
MOL 文件 330786-25-9.mol
更新日期 2024/12/03 15:40:33
330786-25-9 結(jié)構(gòu)式 330786-25-9 結(jié)構(gòu)式

基本信息

中文別名
化合物PCI29732
4-氨基-1-環(huán)戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶
英文別名
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)-
所屬類別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

沸點(diǎn)599.6±50.0 °C(Predicted)
密度1.36±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMF: 20 mg/ml; DMF:PBS (pH 7.2) (1:2): 0.3 mg/ml; DMSO: 10 mg/ml; Ethanol: 5 mg/ml
酸度系數(shù)(pKa)4.24±0.30(Predicted)
形態(tài)粉末
顏色White to off-white

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
防范說(shuō)明P261-P305+P351+P338
4-氨基-1-環(huán)戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-180104-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
330786-25-95mg1000元
2024/11/08HY-180104-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
330786-25-910mM * 1mLin DMSO1100元
2024/11/08HY-180104-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
330786-25-910mg1600元

常見(jiàn)問(wèn)題列表

生物活性
PCI 29732是一種選擇性的、不可逆的Btk抑制劑,IC50為0.5 nM。
靶點(diǎn)
TargetValue
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
體外研究

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).

體內(nèi)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.
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