BIBR1532 is a potent and selective telomerase inhibitor with IC50 of 93 nM. The selectivity of BIBR1532 was assessed in a panel of DNA and RNA polymerases, including HIV reverse transcriptase, showing that none of these enzymes was inhibited at concentrations vastly exceeding the IC50 for telomerase.
|Source||Target Oncol (2015). Figure 3. BIBR1532|
|Method||cell apoptosis assay|
|Cell Lines||MCF-7 cells|
|Incubation Time||24 h|
|Results||The drug combination induced 28.67±2.03 % apoptosis, which is significantly higher than apoptosis caused by 20 μM BIBR1532 alone.|
|Source||Target Oncol (2015). Figure 2. BIBR1532|
|Method||colony formation assay|
|Cell Lines||MCF-7 cells|
|Incubation Time||72 h|
|Results||BIBR1532 and paclitaxel alone inhibited cell colony formation in a dose-dependent manner in MCF-7 cells.|
|Cell lines||JVM13 cells|
|Preparation method||Telomerase activity measurements. Telomerase activity of cell populations was determined using the TeloTaGGG polymerase chain reaction enzyme-linked immunosorbent assay (PCR ELISAPLUS) kit (Roche, Mannheim, Germany) according to the manufacturer’s protocol (telomeric repeat amplification protocol [TRAP] assay). Heat-treated cellular lysates (85°C for 10 minutes) were used as negative controls for each sample. Samples are considered as telomerase positive if the difference in absorbance is higher than 2-fold background activity. WST-1 assays Cells (0.5 to 5*104) were plated as triplicates in complete RPMI 1640 medium with various concentrations of BIBR1532. After 24 to 72 hours, water-soluble tetrazolium (WST-1) (Roche) was 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 was quantified by ELISA reader after 2, 3, and 4 hours of incubation.|
|Concentrations||0 ~ 80 μM|
|Incubation time||24 or 72h|
|Animal models||Human MM xenograft murine model in CB 17 SCID-mice|
|Formulation||phosphate-buffered saline (PBS)|
|Dosages||35 mg/kg daily|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 60 mg/mL|
 Bashash et al. Cancer Invest. Direct short-term cytotoxic effects of BIBR 1532 on acute promyelocytic leukemia cells through induction of p21 coupled with downregulation of c-Myc and hTERT transcription.
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