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BIBR1532

Cat. No. M1676
BIBR1532 Structure
Size Price Availability Quantity
10mM/1mL In DMSO USD 100 In stock
10mg USD 90 In stock
50mg USD 300 In stock
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Quality Control
Biological Activity

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.

Customer Product Validations & Biological Datas
Source Target Oncol (2015). Figure 3. BIBR1532
Method cell apoptosis assay
Cell Lines MCF-7 cells
Concentrations 10 μM
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
Concentrations 10 μM
Incubation Time 72 h
Results BIBR1532 and paclitaxel alone inhibited cell colony formation in a dose-dependent manner in MCF-7 cells.
Protocol
Cell Experiment
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 Experiment
Animal models Human MM xenograft murine model in CB 17 SCID-mice
Formulation phosphate-buffered saline (PBS)
Dosages 35 mg/kg daily
Administration intraperitoneally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 331.36
Formula C21H17NO3
CAS Number 321674-73-1
Purity 98.27%
Solubility DMSO
Storage at -20°C
References

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.
Bashash et al. Cancer Invest. 2012 Jan;30(1):57-64. PMID: 22236190.

Targeted inhibition of telomerase activity combined with chemotherapy demonstrates synergy in eliminating ovarian cancer spheroid-forming cells.
Meng et al. Gynecol Oncol. 2012 Mar;124(3):598-605. PMID: 22115853.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BIBR1532 supplier, Checkpoint, inhibitors

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