BIBR 1532 (Synonyms: Telomerase Inhibitor X) |
رقم الكتالوجGC13636
One-Click Copy Product Info
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BIBR 1532 هو مثبط تيلوميراز قوي وانتقائي وغير تنافسي مع IC 50 من 100 نانومتر في اختبار خالٍ من الخلايا
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 321674-73-1
Sample solution is provided at 25 µL, 10mM.
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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.
| 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: | |
| Cas No. | 321674-73-1 | SDF | |
| المرادفات | Telomerase Inhibitor X | ||
| Chemical Name | 2-[[(E)-3-naphthalen-2-ylbut-2-enoyl]amino]benzoic acid | ||
| Canonical SMILES | CC(=CC(=O)NC1=CC=CC=C1C(=O)O)C2=CC3=CC=CC=C3C=C2 | ||
| Formula | C21H17NO3 | M.Wt | 331.36 |
| الذوبان | ≥ 15.65mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0179 mL | 15.0893 mL | 30.1787 mL |
| 5 mM | 603.6 μL | 3.0179 mL | 6.0357 mL |
| 10 mM | 301.8 μL | 1.5089 mL | 3.0179 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)