中文名称: | PI-3065 | ||||
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英文名称: | PI-3065 | ||||
别名: | 4-(6-((4-(环丙基甲基)哌嗪-1-基)甲基)-2-(5-氟-1H-吲哚-4-基)噻吩并[3,2-d]嘧啶-4-基)吗啉 4-(6-((4-(Cyclopropylmethyl)piperazin-1-yl)methyl)-2-(5-fluoro-1H-indol-4-yl)thieno[3,2-d]pyrimidin-4-yl)morpholine | ||||
CAS No: | 955977-50-1 | 分子式: | C27H31FN6Os | 分子量: | 506.64 |
CAS No: | 955977-50-1 | ||||
分子式: | C27H31FN6Os | ||||
分子量: | 506.64 |
基本信息
产品编号: |
P11740 |
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产品名称: |
PI-3065 |
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CAS: |
955977-50-1 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量: |
506.64 |
-20℃ |
1个月 |
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化学名: |
4-(6-((4-(Cyclopropylmethyl)piperazin-1-yl)methyl)-2-(5-fluoro-1H-indol-4-yl)thieno[3,2-d]pyrimidin-4-yl)morpholine |
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Solubility (25°C): |
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体外:
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DMSO |
50mg/mL warmed with 50ºC water bath (98.68mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内(现配现用): |
1.请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2.5mg/mL(4.93mM);Clear solution |
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此⽅案可获得 ≥ 2.5 mg/mL (4.93mM,饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例,取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中,混合均匀;向上述体系中加⼊ 50 μ L Tween-80,混合均匀;然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。 |
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2.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility:≥2.5mg/mL(4.93mM);Clear solution |
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此⽅案可获得 ≥ 2.5 mg/mL (4.93mM,饱和度未知) 的澄清溶液,此⽅案不适⽤于实验周期在半个⽉以上的实验。以 1mL ⼯作液为例,取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL ⽟⽶油中,混合均匀。 |
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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 |
1.9738mL |
9.8689mL |
19.7379mL |
5mM |
0.3948mL |
1.9738mL |
3.9476mL |
10mM |
0.1974mL |
0.9869mL |
1.9738mL |
生物活性
产品描述 |
一种有效的PI3K p110δ抑制剂。 |
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靶点 |
p110α 910nM (IC50) |
p110β 600nM (IC50) |
p110δ 5nM (IC50) |
体外研究 |
PI-3065 exhibits no inhibition of the growth of 4T1 cells,which do not express detectable levels of p110δ. |
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体内研究 |
PI-3065 (75mg/kg,p.o.) inhibits the growth of 4T1 tumours in the BALB/c mice without obvious body weight loss. |
推荐实验方法(仅供参考)
动物实验: |
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Female WT BALB/c mice are orthotopically inoculated in the mammary fat pad on day 0 with 1×105 4T1 cells.Drug (75mg/kg PI-3065,once daily) or vehicle (0.5% methylcellulose with 0.2% Tween 80) is administered by oral gavage from day -1 (administered 12h prior to tumour cell inoculation).Tumour growth is monitored weekly by caliper measurement or by measuring luminescence using a Xenogen imaging platform.On day 35,mice are euthanized,tumours and peripheral organs extracted for in vitro luminescence measurement,followed by fixation in 4% PFA and H&E staining.KPC mice are allowed to develop advanced lesions of 5-10 mm (determined by ultrasound imaging) before treatment with vehicle or PI3065 for a total of 14 days. |
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 )