BIBR 1532
BIBR 1532
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MK-2206, an allosteric Akt inhibitor, enhances antitumor efficacy.
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.
| On Sale | 1 |
|---|---|
| Cas No. | 321674-73-1 |
| 分子量 | 331.36 |
| 分子式 | C21H17NO3 |
| 别名 | 2-[[(2E)-3-(2-萘基)-1-氧代-2-丁烯基]氨基]苯甲酸 |
| 溶解度 | ≥ 15.65mg/mL in DMSO |
| 储存条件 | Store at -20°C |
| 化学名 | 2-[[(E)-3-naphthalen-2-ylbut-2-enoyl]amino]benzoic acid |
| 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 |
| Canonical SMILES | CC(=CC(=O)NC1=CC=CC=C1C(=O)O)C2=CC3=CC=CC=C3C=C2 |
