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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
4℃
- 保质期:
详见说明
- 英文名:
BIBR 1532
- 库存:
充足
- 供应商:
杭州昊鑫生物
- CAS号:
321674-73-1
- 规格:
10mg
BIBR 1532
BIBR 1532 是一种有效的,选择性的 telomerase 非竞争性抑制剂,IC50 值为 100 nM。
美国medchemexpress(MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
MCE中国是全球领先的科研化学品和生物活性化合物供应商,总部位于美国新泽西。我们的产品范围覆盖各种抑制剂、激动剂、API和化合物库。专业、高效的企业灵魂铸造了在行业的卓越地位。热情和充满活力的研发团队拥有着大量的化学和生物科学家。专注于生物活性化合物,拥有着多年的发展历程和丰富的行业经验。
生物活性
BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay.
IC50 & Target
IC50: 100 nM (telomerase)
体外研究
(In Vitro)
BIBR 1532 non-competitively inhibits telomerase activity[1]. BIBR 1532 inhibits the proliferation of JVM13 leukemia cells with an IC50 of 52 μM, and similar effect also occurs in other leukemia cell lines such as Nalm-1, HL-60, and Jurkat. BIBR 1532 exerts antiproliferative effect on acute myeloid leukemia (AML) with IC50 of 56 μM with no effect on the proliferative capacity of normal hematopoietic progenitor cells[2]. BIBR 1532 (2.5 μM) reduces colony-forming ability, induces telomere length shortening and causes chemotherapeutic sensitization via inhibiting telomerase activity in MCF-7/WT and melphalan-resistant MCF-7/MlnR cell lines[3]. BIBR 1532 is cytotoxic in a dose-dependent manner in T-cell prolymphocytic leukemia (T-PLL)[4]. BIBR 1532 in combination with carboplatin (a chemotherapeutic agent) eliminates ovarian cancer spheroid-forming cells in ES2, SKOV3, and TOV112D cell lines[5].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
331.36
性状
Solid
Formula
C21H17NO3
CAS 号
321674-73-1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro:
DMSO : ≥ 100 mg/mL (301.79 mM)
* "≥" means soluble, but saturation unknown.
配制储备液
浓度溶剂体积质量 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
*
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, 6 months; -20°C, 1 month。-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。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
1.
请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (7.54 mM); Clear solution
2.
请依序添加每种溶剂: 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.54 mM); Clear solution
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文献和实验[1]. Pascolo E, et al. Mechanism of human telomerase inhibition by BIBR1532, a synthetic, non-nucleosidic drug candidate. J Biol Chem. 2002 May 3;277(18):15566-72. [Content Brief]
[2]. El-Daly H, et al. Selective cytotoxicity and telomere damage in leukemia cells using the telomerase inhibitor BIBR1532. Blood. 2005 Feb 15;105(4):1742-9. [Content Brief]
[3]. Ward RJ, et al. Pharmacological telomerase inhibition can sensitize drug-resistant and drug-sensitive cells to chemotherapeutic treatment. Mol Pharmacol. 2005 Sep;68(3):779-86. [Content Brief]
[4]. A Röth, et al. Short telomeres and high telomerase activity in T-cell prolymphocytic leukemia. Leukemia. 2007 Dec;21(12):2456-62. [Content Brief]
[5]. Meng E, et al. Targeted inhibition of telomerase activity combined with chemotherapy demonstrates synergy in eliminating ovarian cancer spheroid-forming cells. Gynecol Oncol. 2012 Mar;124(3):598-605. [Content Brief]
BIBR1532 that is a selective, non-nucleosidic inhibitor of the catalytic component hTERT. Treatment of cancer cells with this compound leads to progressive telomere shortening, consecutive telomere dysfunction, and finally growth arrest after a lag
Screening of Telomerase Inhibitors
(G-quadruplex-interactive compound), BIBR1532 (non-nucleosidic reverse transcriptase inhibitor), 2′-O-methyl RNA, and peptide nucleic acids (PNAs; hTR antisense oligonucleotides). To determine minimal effective concentrations for telomerase inhibition
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