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
A potent telomerase inhibitor
Cas No.:321674-73-1
Sample solution is provided at 25 µL, 10mM.
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BIBR 1532 is a novel, specific telomerase inhibitor with IC50 of 93 nM [1].
It has been reported that BIBR 1532 inhibited the reverse transcriptase of telomerase, hTERT, and shortened the length of the telomerase to suppress human cancer cell proliferation [1]. In pre-B acute lymphoblastic leukemia cells, BIBR1532 suppressed c-Myc and hTERT expression in a concentration-dependent manner to inhibit telomerase activity, and high doses of BIBR1532 could induce apoptosis by elevating p73, Bax/Bcl-2 and caspase-3 activation [2]. In NB4 leukemic cells, combined treatments with BIBR 1532 and arsenic trioxide suppressed cell proliferative capacity and inhibited telomerase activity probably via transcriptional suppression of c-Myc and hTERT. [4]
References:
[1]. Damm, K.; Hemmann, U.; Garin-Chesa, P.; Hauel, N.; Kauffman, I.; Priepke, H.; Niestroj, C.; Daiber, C.; Enenkel, B.; Guilliard, B.; Lauritsch, I.; Muller, E.; Pascolo, E.; Sauter, G.; Pantic, M.; Martens, U. M.; Wenz, C.; Linger, J.; Kraut, N.; Rettig, W. J.;Schnapp, A. A highly selective telomerase inhibitor limiting human cancer cell proliferation. EMBO J. 2001, 20, 6958−6968.
[2]. Bashash D1, Ghaffari SH, Mirzaee R, Alimoghaddam K, Ghavamzadeh A. Telomerase inhibition by non-nucleosidic compound BIBR1532 causes rapid cell death in pre-B acute lymphoblastic leukemia cells. Leuk Lymphoma. 2013 Mar;54[4]:561-8. doi: 10.3109/10428194.2012.704034. Epub 2012 Sep 28.
[3]. Bashash D1, Ghaffari SH, Zaker F, Kazerani M, Hezave K, Hassani S, Rostami M, Alimoghaddam K, Ghavamzadeh A. Anticancer Agents Med Chem. 2013 Sep;13(7):1115-25. BIBR 1532 increases arsenic trioxide-mediated apoptosis in acute promyelocytic leukemia cells: therapeutic potential for APL.
| Kinase experiment [1]: | |
|
Conventional telomerase assay |
For the direct telomerase assay with the endogenous telomerase, 10 μL of telomerase-enriched extract was mixed with different concentrations of BIBR 1532 in a final volume of 20 μL. After 15-minute preincubation on ice, 20 μL of the reaction mixture was added, and the reaction was initiated by transferring the tubes to 37 °C. The final concentrations in the reaction mixture were 25 mM Tris-Cl (pH 8.3), 1 mM MgCl2, 1 mM EGTA, 1 mM dATP, 1 mM dTTP, 6.3 μM cold dGTP, 15 μCi [α-32P]dGTP (3000 Ci/mmol), 1.25 mM spermidine, 10 units of RNasin, 5 mM 2-mercaptoethanol, and 2.5 μM TS-primer (5'-AATCCGTCGAGCAGAGTT). |
| Cell experiment [2]: | |
|
Cell lines |
Nalm-6 cells |
|
Preparation method |
The solubility of this compound in DMSO is > 15.65 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
10, 30, 60 and 90 μ M; for 48 hrs |
|
Applications |
In Nalm-6 cells, BIBR 1532 at the concentrations of 30, 60 and 90 μM inhibited DNA synthesis rates by 10, 17 and 28%, respectively. MTT assay analysis showed that BIBR 1532 concentration-dependently reduced the metabolic activity of Nalm-6 cells (15, 30 and 44% at the concentrations of 30, 60 and 90 μ M, respectively). At the doses of 10 and 30 μM, BIBR 1532 partially inhibited telomerase activity while at the higher doses, i.e. 60 and 90 μM, BIBR 1532 resulted in marked telomerase inhibition. |
|
References: [1]. Pascolo E, Wenz C, Lingner J, Hauel N, Priepke H, Kauffmann I, Garin-Chesa P, Rettig WJ, Damm K, Schnapp A. Mechanism of human telomerase inhibition by BIBR1532, a synthetic, non-nucleosidic drug candidate. J Biol Chem. 2002 May 3;277(18):15566-72. [2]. Bashash D1, Ghaffari SH, Mirzaee R, Alimoghaddam K, Ghavamzadeh A. Telomerase inhibition by non-nucleosidic compound BIBR1532 causes rapid cell death in pre-B acute lymphoblastic leukemia cells. Leuk Lymphoma. 2013 Mar;54[4]:561-8. | |
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0179 mL | 15.0893 mL | 30.1787 mL |
| 5 mM | 0.6036 mL | 3.0179 mL | 6.0357 mL |
| 10 mM | 0.3018 mL | 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
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet