330786-25-9

中文名称 4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶

英文名称 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 2024/04/07 11:18:39

330786-25-9 结构式

基本信息物理化学性质安全数据 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) 常见问题列表

基本信息

中文别名

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
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)-

所属类别

生物化工：激动剂抑制剂

物理化学性质

沸点599.6±50.0 °C(Predicted)

密度1.36±0.1 g/cm3(Predicted)

储存条件-20°C储存

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

酸度系数(pKa)4.24±0.30(Predicted)

形态粉末

颜色White to off-white

安全数据

危险性符号(GHS)

GHS07

警示词警告

危险性描述H302-H315-H319-H335

防范说明P261-P305+P351+P338

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)

报价日期	产品编号	产品名称	CAS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
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	10mg	1600元

常见问题列表

生物活性

PCI 29732是一种选择性的、不可逆的Btk抑制剂，IC50为0.5 nM。

靶点

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

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.