GLPBio

BIBR 1532

Catalog No.: GC13636Purity:>99.50%Synonyms: Telomerase Inhibitor X
COASDSData Sheet
BIBR 1532 is a potent small molecule inhibitor of human telomerase, with an IC50 value of 5µM for telomerase inhibition. BIBR 1532 causes telomeres to shorten and reduces tumor cell proliferation.

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BIBR 1532
Cas No.: 321674-73-1
10mM (in 1mL DMSO)In Stock
$55.00
1
1mgIn Stock
$14.00
1
5mgIn Stock
$31.00
1
10mgIn Stock
$50.00
1
25mgIn Stock
$115.00
1
50mgIn Stock
$195.00
1
100mgIn Stock
$307.00
1
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Description

BIBR 1532 is a potent small molecule inhibitor of human telomerase, with an IC50 value of 5µM for telomerase inhibition. BIBR 1532 causes telomeres to shorten and reduces tumor cell proliferation[1].

In vitro, BIBR 1532 (30µM; 48h) increases arsenic trioxide-mediated apoptosis in acute promyelocytic leukemia cells[2]. BIBR 1532 (20μM or 40μM; 72h) combined with radiotherapy induces ferroptosis in NSCLC cells and activates cGAS-STING pathway to promote anti-tumor immunity[3].

In vivo, BIBR 1532 (166-1326pg/μl; twice; intravitreal injection) specifically induces the suppression of choroidal neovascularization (CNV) in mice through the inhibition of telomerase[4]. In a mouse xenograft model, BIBR 1532 (1.5mg/kg; 3 days; i.p.) treatment synergized with ionizing radiation (IR) at nontoxic dose levels promoted the antitumor efficacy of IR without toxicity to hematologic and internal organs[5].

References:
[1] Barma DK, Elayadi A, Falck JR, et al. Inhibition of telomerase by BIBR 1532 and related analogues. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1333-6.
[2] Bashash D, Ghaffari SH, Zaker F, et al. BIBR 1532 increases arsenic trioxide-mediated apoptosis in acute promyelocytic leukemia cells: therapeutic potential for APL. Anticancer Agents Med Chem. 2013 Sep;13(7):1115-25.
[3] Bao Y, Pan Z, Zhao L, et al. BIBR1532 combined with radiotherapy induces ferroptosis in NSCLC cells and activates cGAS-STING pathway to promote anti-tumor immunity. J Transl Med. 2024 May 30;22(1):519.
[4] Kumar A, Nagasaka Y, Jayananthan V, et al. Therapeutic targeting of telomerase ameliorates experimental choroidal neovascularization. Biochim Biophys Acta Mol Basis Dis. 2024 Jun;1870(5):167156.
[5] Ding X, Cheng J, Pang Q, et al. BIBR1532, a Selective Telomerase Inhibitor, Enhances Radiosensitivity of Non-Small Cell Lung Cancer Through Increasing Telomere Dysfunction and ATM/CHK1 Inhibition. Int J Radiat Oncol Biol Phys. 2019 Nov 15;105(4):861-874.

Protocol

Cell experiment [1]:

Cell lines

NB4 (human APL cell line) cells

Preparation Method

NB4 (human APL cell line) cells were seeded into 12-well cell culture plates and treated with desired concentrations of ATO (arsenic trioxide), BIBR 1532, and the combination of BIBR 1532 (30µM) with ATO (0.5 and 1µM) for 48h. The cell suspensions were then washed in cold phosphate-buffered saline (PBS) and the cell density was adjusted to approximately 5×10⁵cells/mL. A volume of 1mL was used for each assay. One microliter of the Hoechst 33342 stock solution (5.0mg/mL in water) and 1µL of the propidium iodide stock solution (1.0mg/mL in water) were added to each 1mL of cell suspension. After 20min, the stained cells were evaluated by flow cytometry, with excitation/emission wavelengths of approximately 350/461nm for Hoechst 33342 and 535/617nm for propidium iodide. Subsequently, the data were analyzed using FlowMax software.

Reaction Conditions

30µM; 48h

Applications

BIBR 1532 increases arsenic trioxide-mediated apoptosis in acute promyelocytic leukemia cells.
Animal experiment [2]:

Animal models

female athymic nude mice

Preparation Method

Calu-3 cells (5 × 10⁶) were injected subcutaneously into the lower limbs of female athymic nude mice. When the volume of a transplanted tumor reached 200mm³, the mice were treated with BIBR 1532 for 3 days (1.5mg/kg and saline as vehicle control, intraperitoneal injection), followed by 10 Gy of radiation over 5 fractions. The tumor volume of xenografts was measured with calipers every 3 days. After the mice were sacrificed, sections of tumors were excised for hematoxylin and eosin staining, immunohistochemical staining of p-ATM, and TUNEL assays.

Dosage form

1.5mg/kg; 3 days; i.p.

Applications

In a mouse xenograft model, BIBR 1532 treatment synergized with ionizing radiation (IR) at nontoxic dose levels promoted the antitumor efficacy of IR without toxicity to hematologic and internal organs.

References:
[1] Bashash D, Ghaffari SH, Zaker F, et al. BIBR 1532 increases arsenic trioxide-mediated apoptosis in acute promyelocytic leukemia cells: therapeutic potential for APL. Anticancer Agents Med Chem. 2013 Sep;13(7):1115-25.
[2] Ding X, Cheng J, Pang Q, et al. BIBR1532, a Selective Telomerase Inhibitor, Enhances Radiosensitivity of Non-Small Cell Lung Cancer Through Increasing Telomere Dysfunction and ATM/CHK1 Inhibition. Int J Radiat Oncol Biol Phys. 2019 Nov 15;105(4):861-874.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
321674-73-1
Synonyms
Telomerase Inhibitor X
Chemical Name
2-[[(E)-3-naphthalen-2-ylbut-2-enoyl]amino]benzoic acid
SMILES
CC(=CC(=O)NC1=CC=CC=C1C(=O)O)C2=CC3=CC=CC=C3C=C2
Molecular Formula
C21H17NO3
Molecular Weight
331.36
Solubility
≥ 15.65mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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