| 中文名称: | BIX-01294 促销 | ||||
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| 英文名称: | BIX-01294 | ||||
| 别名: | N-(1-Benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine | ||||
| CAS No: | 935693-62-2 | 分子式: | C28H38N6O2 | 分子量: | 490.64 |
| CAS No: | 935693-62-2 | ||||
| 分子式: | C28H38N6O2 | ||||
| 分子量: | 490.64 | ||||
基本信息
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产品编号：B10770 |
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产品名称：BIX-01294 |
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CAS: |
935693-62-2 |
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： |
490.64 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
100mg/mL (166.66mM) |
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Ethanol |
100mg/mL (166.66mM) |
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Water |
100mg/mL (166.66mM) |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
1.6666mL |
8.3331mL |
16.6661mL |
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5mM |
0.3333mL |
1.6666mL |
3.3332mL |
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10mM |
0.1667mL |
0.8333mL |
1.6666mL |
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50mM |
0.0333mL |
0.1667mL |
0.3333mL |
生物活性
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产品描述 |
一种 G9a 组蛋白甲基转移酶 (G9a Histone Methyltransferase) 抑制剂，IC50 值为 1.9μM。 |
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靶点/IC50 |
G9a |
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2.7μM |
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体外研究 |
BIX-01294 (2μM; 48 h) selectively inhibits recurrent tumor cell growth.BIX-01294 (1μM) leads to a marked increase in phosphorylation of S345 of MLKL.BIX-01294 (1μM) significantly upregulates the canonical p53 targets Cdkn1a (p21) and Gadd45a in recurrent tumor cell lines.BIX-01294 (1μM; 6 days) causes the reduction in H3K9me2 levels in primary and recurrent tumor cells.BIX-01294 leads to necroptotic cell death in recurrent tumor cells. Necrostatin-1 (30μM) partially reverses cell death induced by BIX-01294 (750nM; 24 h).BIX-01294 (4.1μM; for 2 days) causes around a 20% reduction, concomitant with a comparable increase in the unmodified H3K9 fragment in H3K9me2 in mouse ES cells. BIX-01294 causes pronounced reduction in H3K9me2 and a small decrease for H3K9me3 and H3K9me1 in wild-type ES cells.BIX-01294 has no inhibition of the other histone methyltransferases even at concentrations of 45μM. BIX-01294 does not affect SUV39H1 (H320R) and PRMT1 within the tested concentration range (up to 10μM).BIX-01294 inhibits G9a in an uncompetitive manner with S-adenosyl-methionine (SAM).BIX-01294 (1µg/mL) causes reduction in the BrdU incorporation of fetal PASMCs. BIX-01294 treatment decreases the PASMCs migration induced by PDGF. Cell Viability Assay |
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Cell Line: |
Primary or recurrent tumor cells |
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Concentration: |
2μM |
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Incubation Time: |
48 hours |
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Result: |
Selectively inhibited recurrent tumor cell growth. |
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体内研究 |
BIX-01294 (10mg/kg; IP; three times a week for 2 weeks) significantly reduces tumor growth and tumor burden in recurrent tumor cells. Primary tumor growth is not inhibited. |
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Animal Model: |
Female MMTV-rtTA;TetO-Her2/neu (MTB;TAN) and TetO-Her2/neu (TAN) mice with recurrent or primary tumor cells |
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Dosage: |
10mg/kg |
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Administration: |
IP;three times a week for 2 weeks |
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Result: |
Significantly reduced tumor growth and tumor burden in recurrent tumor cells.Primary tumor growth was not inhibited. Slowed the growth of orthotopic recurrent tumors in athymic nude recipients. |
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推荐实验方法(仅供参考)
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激酶实验： |
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HMTase实验 |
在涂有Neutravidin的白色不透明384孔板中进行解离增强镧系荧光免疫分析（DELFIA）。实验化合物在含4% DMSO的12μg/ml 50mM Tris-HCl pH 8.5中稀释，每孔分配10μl。空白和对照孔只有化合物缓冲液。10μg/ml GST-G9a和40μM SAM在50mM Tris HCl pH 8.5/10mM DTT 中稀释，然后加入20μL。空白孔只有Tris/DTT缓冲液。加入溶于50mM Tris pH 8.5，体积为10μl的800nM H3(1-20)-cysbiotin 底物，开始反应，在室温下温育60分钟。使用100μl 洗涤缓冲液洗涤实验板3次。然后实验板的每孔中加入含5ng α-2X-二甲基-H3-K9 和 5ng 山羊抗兔Eu螯合物的50μl 荧光免疫(FI) 缓冲液，在室温下再温育1小时。使用100μl洗涤缓冲液 洗涤实验板3次，每孔加入50μl增强液。45分钟后在Viewlux微孔板成像仪成像15秒，测量时间分辨荧光。 |
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 )
