4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶 CAS#: 330786-25-9

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

生物活性靶点体外研究体内研究用途与合成方法 MSDS 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) 上下游产品信息

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
中文同义词	4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶;化合物PCI29732;PCI 29732,BTK抑制剂
英文名称	PCI 29732
英文同义词	PCI 29732;4-Amino-1-cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine;1-Cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine;PCI 29732 (This product is only available in Japan.);CS-2698;PCI 29732;PCI29732;PCI-29732;1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 1-cyclopentyl-3-(4-phenoxyphenyl)-;cytotoxicity,Bruton tyrosine kinase,Inhibitor,Btk,ABCG2,reversible,PCI 29732,BCR,inhibit,B-cell,BCRP,oral,Breast cancer resistance protein
CAS号	330786-25-9
分子式	C22H21N5O
分子量	371.43
EINECS号
相关类别
Mol文件	330786-25-9.mol
结构式

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

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.

安全信息

MSDS信息

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
2024/04/30	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

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