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BIBR 1532

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Chemical Structure| 321674-73-1 同义名 : Telomerase Inhibitor X
CAS号 : 321674-73-1
货号 : A381410
分子式 : C21H17NO3
纯度 : 99%+
分子量 : 331.365
MDL号 : MFCD11112195
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(316.87 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Telomerase

    Telomerase, IC50:100 nM
描述 BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay[1]. BIBR 1532 inhibits telomerase activity in a non-competitive manner[1]. BIBR 1532 reduces the proliferation of JVM13 leukemia cells, achieving an IC50 of 52 μM, a similar inhibition observed in other leukemia lines like Nalm-1, HL-60, and Jurkat. BIBR 1532's antiproliferative effects on acute myeloid leukemia (AML) are noted with an IC50 of 56 μM, while it does not affect the proliferative ability of normal hematopoietic progenitor cells[2]. At a concentration of 2.5 μM, BIBR 1532 diminishes colony-forming ability, induces telomere shortening, and sensitizes cells to chemotherapy by inhibiting telomerase activity in both MCF-7/WT and MCF-7/MlnR cell lines resistant to melphalan[3]. BIBR 1532 exhibits dose-dependent cytotoxicity in T-cell prolymphocytic leukemia (T-PLL)[4]. When combined with carboplatin, BIBR 1532 eradicates spheroid-forming ovarian cancer cells in ES2, SKOV3, and TOV112D cell lines[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.02mL

0.60mL

0.30mL

15.09mL

3.02mL

1.51mL

30.18mL

6.04mL

3.02mL
参考文献

[1]Pascolo E, et al. Mechanism of human telomerase inhibition by BIBR1532, a synthetic, non-nucleosidic drug candidate. J Biol Chem. 2002 May 3;277(18):15566-72.

[2]El-Daly H, et al. Selective cytotoxicity and telomere damage in leukemia cells using the telomerase inhibitor BIBR1532. Blood. 2005 Feb 15;105(4):1742-9.

[3]Ward RJ, et al. Pharmacological telomerase inhibition can sensitize drug-resistant and drug-sensitive cells to chemotherapeutic treatment. Mol Pharmacol. 2005 Sep;68(3):779-86.

[4]A Röth, et al. Short telomeres and high telomerase activity in T-cell prolymphocytic leukemia. Leukemia. 2007 Dec;21(12):2456-62.

[5]Meng E, et al. Targeted inhibition of telomerase activity combined with chemotherapy demonstrates synergy in eliminating ovarian cancer spheroid-forming cells. Gynecol Oncol. 2012 Mar;124(3):598-605.