中文名称: | BIBR 1532 | ||||
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英文名称: | BIBR 1532 | ||||
别名: | 2-[[(2E)-3-(2-萘基)-1-氧代-2-丁烯基]氨基]苯甲酸;BIBR 1532 国华试剂 (E)-2-(3-(naphthalen-2-yl)but-2-enamido)benzoic acid | ||||
CAS No: | 321674-73-1 | 分子式: | C21H17NO3 | 分子量: | 331.36 |
CAS No: | 321674-73-1 | ||||
分子式: | C21H17NO3 | ||||
分子量: | 331.36 |
基本信息
产品编号:B10725 |
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产品名称:BIBR 1532 |
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CAS: |
321674-73-1 |
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 |
331.36 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
66mg/mL (199.17mM) |
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Ethanol |
3mg/mL (9.05mM) |
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Water |
Insoluble |
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体内(现配现用) |
5% DMSO+corn oil |
10mg/mL |
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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 |
3.0179mL |
15.0893mL |
30.1787mL |
5mM |
0.6036mL |
3.0179mL |
6.0357mL |
10mM |
0.3018mL |
1.5089mL |
3.0179mL |
50mM |
0.0604mL |
0.3018mL |
0.6036mL |
生物活性
产品描述 |
一种有效的,选择性的 telomerase 非竞争性抑制剂,IC50 值为 100nM。 |
靶点/IC50 |
Telomerase |
100nM |
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体外研究 |
BIBR 1532 non-competitively inhibits telomerase activity. BIBR 1532 inhibits the proliferation of JVM13 leukemia cells with an IC50 of 52μM, and similar effect also occurs in other leukemia cell lines such as Nalm-1, HL-60, and Jurkat. BIBR 1532 exerts antiproliferative effect on acute myeloid leukemia (AML) with IC50 of 56μM with no effect on the proliferative capacity of normal hematopoietic progenitor cells. BIBR 1532 (2.5μM) reduces colony-forming ability, induces telomere length shortening and causes chemotherapeutic sensitization via inhibiting telomerase activity in MCF-7/WT and melphalanresistant MCF-7/MlnR cell lines. BIBR 1532 is cytotoxic in a dose-dependent manner in T-cell prolymphocytic leukemia (TPLL). BIBR 1532 in combination with carboplatin (a chemotherapeutic agent) eliminates ovarian cancer spheroid-forming cells in ES2, SKOV3, and TOV112D cell lines. |
推荐实验方法(仅供参考)
激酶实验: |
For the direct telomerase assay with the endogenous telomerase, 10μL of telomerase-enriched extract is mixed with different concentrations of BIBR1532 in a final volume of 20μL. After 15-minute preincubation on ice, 20μL of the reaction mixture is added, and the reaction is initiated by transferring the tubes to 37℃. The final concentrations in the reaction mixture are 25mM Tris-Cl (pH 8.3), 1mM MgCl2, 1mM EGTA, 1mM dATP, 1mM dTTP, 6.3μM cold dGTP, 15μCi [α-32P]dGTP (3000 Ci/mmol; NEN), 1.25mM spermidine, 10 units of RNasin, 5mM 2-mercaptoethanol, and 2.5μM TS-primer (5'-AATCCGTCGAGCAGAGTT). For the recombinant enzyme, 1-7μL of affinity-purified telomerase (containing less than 0.025μM hTERT) are assayed in a final volume of 40μL containing 50mM Tris acetate (pH 8.5), 50mM KCl, 1mM MgCl2, 1mM spermidine, 5mM 2-mercaptoethanol, 1mM dATP, 1mM dTTP, 2.5μM dGTP, 15μCi of [α-32P]dGTP (3000 Ci/mmol) and 2.5μM (TTAGGG)3. The reaction is initiated by incubation at 37℃ for 2 hours and stopped by addition of 50μL of RNase mix (0.1mg/mL RNaseA-100u/mL RNaseT1 in 10mM Tris-Cl (pH 8.3) and 20 mm EDTA) and incubation for 20 min at 37℃. Samples are deproteinated by adding 50μL of 0.3mg/m proteinase K in 10mM Tris-Cl (pH 8.3) and 0.5% w/v SDS, for a 30-minute incubation at 37℃. DNA is recovered by phenol extraction and ethanol precipitation, and the extension products are analyzed on an 8% (endogenous telomerase) or 12% (recombinant telomerase) polyacrylamide-urea gel. Dried gels are exposed to a Kodak phosphorimager screen, and the results are analyzed. |
细胞实验: |
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Cells are plated as triplicates in complete RPMI 1640 medium with various concentrations of BIBR1532. After 24 to 72 hours,water-soluble tetrazolium (WST-1) is added, which is transformed into formazan by mitochondrial reductase systems. The increase in the number of viable cells results in an increase of activity of mitochondrial dehydrogenases, leading to an increase of formazan dye formed, which is quantified by ELISA reader after 2, 3, and 4 hours of incubation. |
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 )