中文名称: | PCI29732 | ||||
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英文名称: | PCI29732 | ||||
别名: | 4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶 PCI29732 | ||||
CAS No: | 330786-25-9 | 分子式: | C22H21N5O | 分子量: | 371.44 |
CAS No: | 330786-25-9 | ||||
分子式: | C22H21N5O | ||||
分子量: | 371.44 |
基本信息
产品编号:P11250 |
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产品名称:PCI29732 |
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CAS: |
330786-25-9 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
459.91 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
74mg/mL (199.23mM) |
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Ethanol |
4mg/mL (10.76mM) |
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Water |
Insoluble |
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体内(现配现用) |
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<1mg/ml表示微溶或不溶。 |
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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。 |
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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。 |
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靶点/IC50 |
BLK |
Bmx |
EGFR |
YES |
0.5nM |
0.8nM |
5.6nM |
6.5nM |
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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). |
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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. |
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Animal Model: |
5-6 weeks old athymic nude mice (bearing H460/MX20 cells) |
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Dosage: |
20 mg/kg (combination with Topotecan; every 3 d × 5 times, i.p.,3mg/kg; topotecan was given 1h after PCI29732 administration) |
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Administration: |
P.o.;every 3 d × 5 times |
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Result: |
Significant reductions in tumor weight and volume were observed in the group treated with PCI29732 in combination with Topotecan. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )