中文名称: BIBR 1532
英文名称: BIBR 1532
CAS No: 321674-73-1
分子式: C21H17NO3
分子量: 331.36
B10725 BIBR 1532 ≥98% (psaitong)
包装规格:
10mg 50mg 100mg in glass bottle
溶解性:
溶于DMSO(≥ 100 mg/mL)
产品描述:

基本信息

产品编号:B10725

产品名称:BIBR 1532

CAS:

321674-73-1

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C21H17NO3

溶于液体

-80℃

六个月

分子量

331.36

-20℃

一个月

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

66mg/mL (199.17mM)

Ethanol

3mg/mL (9.05mM)

Water

Insoluble

体内(现配现用)

5% DMSO+corn oil

10mg/mL

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

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
(Cell-free assay)

100nM

 

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:

 

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.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
搜索质检报告(COA)
参考文献 & 客户发表文献

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

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

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 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):