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PCI29732  ≥98%

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(≥53mg/ml）
产品描述：基本信息 产品编号：P11250 产品名称：PCI29732 CAS: 330786-25-9   储存条件 粉末 -20℃ 四年     分子式： C22H21N5O 溶于液体 -80℃ 六个月 分子量 459.91 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 74mg/mL (199.23mM) Ethanol 4mg/mL (10.76mM) Water Insoluble 体内（现配现用）     ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.6923mL 13.4615mL 26.9230mL 5mM 0.5385mL 2.6923mL 5.3846mL 10mM 0.2692mL 1.3461mL 2.6923mL 50mM 0.0538mL 0.2692mL 0.5385mL   生物活性 产品描述 一种有效的可逆BTK抑制剂。 靶点/IC50 BLK (Cell-free assay) Bmx(Cell-free assay) EGFR(Cell-free assay) YES(Cell-free assay) 0.5nM 0.8nM 5.6nM 6.5nM 体外研究 PCI29732 shows cytotoxicity in different cells. The IC50 values are 7.94μM for S1, 7.79μM for S1-MI-80, 6.55μM for H460, 6.34μM for H460/MX20, 6.14μM for KB, 6.02μM for KBv200, 12.45μM for HEK293/pcDNA3, 14.58μM for HEK293-ABCG2-482-R2, and 13.24μM 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 antitumor efficacy of substrate chemotherapeutic agents. PCI 29732 (20mg/kg; p.o.; every 3 d × 5 times) enhances the anticancer efficacy of Topotecan in the H460/MX20 cell xenograft nude mice mode. 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.,3mg/kg; topotecan was given 1h 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.
保存条件：-20℃

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