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CAS No.: 321674-73-1

BIBR 1532 Catalog No. CSN18209

Synonyms: Telomerase Inhibitor X

BIBR 1532 is a non-competitive inhibitor of telomerase with IC50 of 100 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Telomerase

IC50:100nM
描述BIBR 1532 exhibits an non-competitive inhibitory effect on telomerase activity. In JVM13 leukemia cell line, BIBR 1532 shows an antiproliferative effect in a dose-dependent range with IC₅₀ of 52 μM, and similar results are also observed in other leukemia cell lines including Nalm-1, HL-60, and Jurkat. In addition, BIBR 1532 results in a direct antiproliferative effect on acute myeloid leukemia (AML) with IC₅₀ of 56 μM without affecting the proliferative capacity of normal hematopoietic progenitor cells. BIBR 1532 (2.5 μM) reduces colony-forming ability, and induces telomere length shortening as well as chemotherapeutic sensitization by inhibiting telomerase activity in MCF-7/WT and melphalan-resistant MCF-7/Mln cell lines. In T-cell prolymphocytic leukemia (T-PLL), BIBR 1532 shows selective cytotoxic effects in a dose-dependent manner and BIBR 1532-treated cells also demonstrates nuclear condensation and formation of apoptotic bodies morphologically compatible with apoptosis. A recent study shows that combination treatment of BIBR 1532 and chemotherapeutic agents carboplatin results in a potential synergy for eliminateing ovarian cancer spheroid-forming cells in ES2, SKOV3, and TOV112D cell lines.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human HeLa cells	-	Function assay	2 h	Inhibition of telomerase in human HeLa cells after 2 hrs by [alpha-32P]dGTP incorporation assay, IC50=93 nM	22413845
human MDA-MB-231 cells	-	Function assay	24 h	Inhibition of telomerase in human MDA-MB-231 cells after 24 hrs by TRAP-PCR-ELISA, IC50=0.17 μM	25965778
human MGC803 cells	-	Function assay	24 h	Inhibition of telomerase in human MGC803 cells after 24 hrs by TRAP-PCR-ELISA, IC50=0.28 μM	25554922

动物研究
剂量
Nude Mice: 1 mg/kg - 2 mg/kg^[2] (i.p.) Mice: 100 mg/kg^[3] (p.o.)

给药途径
i.p., p.o.
参考文献

动物研究
剂量	Nude Mice: 1 mg/kg - 2 mg/kg^[2] (i.p.) Mice: 100 mg/kg^[3] (p.o.)
给药途径	i.p., p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0179 mL
- 15.0893 mL
- 30.1787 mL
- 5 mM
- 0.6036 mL
- 3.0179 mL
- 6.0357 mL
- 10 mM
- 0.3018 mL
- 1.5089 mL
- 3.0179 mL

技术信息

CAS号

321674-73-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H17NO3

运输

蓝冰

分子量

331.36

别名

Telomerase Inhibitor X

溶解度

DMSO	66.0 mg/mL (199.2 mM)
Water	Insoluble
Ethanol	3.0 mg/mL (9.1 mM)

动物实验配方

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BIBR 1532 Catalog No. CSN18209

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