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].
体外研究
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].
BIBR 1532 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HeLa cells
20 µM
10 days
To investigate the effect of BIBR1532 on HeLa cell proliferation, the results showed that BIBR1532 significantly inhibited cell proliferation
Cell Death Dis. 2019 Jul 11;10(7):527.
EBV-positive lymphoblastoid cell lines and Burkitt’s lymphoma cell lines
30 µM
16, 24, 36, 48 and 72 hours
To evaluate the effect of BIBR on cell proliferation and apoptosis.
Cell Death Dis. 2016 Dec 29;7(12):e2562.
Primary mouse hepatocytes
20 µM
24 hours
To assess the effects on SASP expression and signaling pathways.
Cell Mol Life Sci. 2024 Apr 30;81(1):200.
MCF-7 and MDA-MB 231 cells
50 µM
48 hours
The purpose was to assess apoptosis induction; results indicated a decrease in apoptotic cells when treated with BIBR 1532.
Cancer Cell Int. 2014 Jul 4;14:60.
MCF-7 cells
20 µM
To investigate the effect of BIBR1532 on MCF-7 cell proliferation, the results showed that BIBR1532 significantly inhibited cell proliferation
Cell Death Dis. 2019 Jul 11;10(7):527.
BIBR 1532 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Balb/c mice
4T1 cell xenograft breast cancer model
IntratumOral injection
10 mg/kg/d
Once daily for 14 days
To investigate the effect of BIBR1532 on 4T1 cell xenograft breast cancer model, the results showed that BIBR1532 significantly inhibited tumor growth
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