BIBR 1532
(Synonyms: 2-[[(2E)-3-(2-萘基)-1-氧代-2-丁烯基]氨基]苯甲酸) 目录号 : GC13636
BIBR 1532是一种强效的小分子人类端粒酶抑制剂，对端粒酶的抑制作用的IC50值为5μM。BIBR 1532会导致端粒缩短并减少肿瘤细胞的增殖。
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.
BIBR 1532是一种强效的小分子人类端粒酶抑制剂，对端粒酶的抑制作用的IC50值为5μM。BIBR 1532会导致端粒缩短并减少肿瘤细胞的增殖[1]。
在体外实验中，BIBR 1532（30µM; 48h）增加了急性早幼粒细胞白血病细胞中三氧化二砷介导的凋亡[2]。BIBR 1532（20µM或40µM; 72h）与放疗联合使用可在非小细胞肺癌（NSCLC）细胞中诱导铁死亡，并激活cGAS-STING通路以促进抗肿瘤免疫[3]。
在体内实验中，BIBR 1532（166-1326pg/µl; 两次; 眼内注射）通过抑制端粒酶特异性地诱导小鼠脉络膜新生血管（CNV）的抑制[4]。在小鼠异种移植模型中，非毒性剂量水平的BIBR 1532（1.5mg/kg; 3天; 腹腔注射）治疗与电离辐射（IR）协同作用，增强了IR的抗肿瘤效果，且对造血系统和内脏器官无毒性[5]。
| 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 | |
| 别名 | 2-[[(2E)-3-(2-萘基)-1-氧代-2-丁烯基]氨基]苯甲酸 | ||
| 化学名 | 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 | ||
| 分子式 | C21H17NO3 | 分子量 | 331.36 |
| 溶解度 | ≥ 15.65mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
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