Free shipping on all orders over $ 500

BIBR1532

Cat. No. M1676
BIBR1532 Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 80  USD80 In stock
5mg USD 60  USD60 In stock
10mg USD 90  USD90 In stock
50mg USD 340  USD340 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

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 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.

Chemical Information
Molecular Weight 331.36
Formula C21H17NO3
CAS Number 321674-73-1
Purity 98.33%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

[1] 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.

[2] Meng et al. Gynecol Oncol. Targeted inhibition of telomerase activity combined with chemotherapy demonstrates synergy in eliminating ovarian cancer spheroid-forming cells.

Related Checkpoint Products
WAY-239320

WAY-239320 is a Chk1 inhibitor

Prexasertib dimesylate

Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM.

Prexasertib

Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM.

GDC-0575 dihydrochloride

GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.

CCT244747

CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.

  Catalog
Abmole Inhibitor Catalog




Keywords: BIBR1532 supplier, Checkpoint, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.