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产品名称 | Telomerase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
4',7-Dimethoxyisoflavone | ✔ | 97% | |||||||||||||||||
BIBR 1532 |
+++
Telomerase, IC50: 100 nM |
99%+ | |||||||||||||||||
Costunolide |
++
Telomerase (MDA-MB-231), IC50: 65 μM Telomerase (MCF-7), IC50: 90 μM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay[1]. BIBR 1532 inhibits telomerase activity in a non-competitive manner[1]. BIBR 1532 reduces the proliferation of JVM13 leukemia cells, achieving an IC50 of 52 μM, a similar inhibition observed in other leukemia lines like Nalm-1, HL-60, and Jurkat. BIBR 1532's antiproliferative effects on acute myeloid leukemia (AML) are noted with an IC50 of 56 μM, while it does not affect the proliferative ability of normal hematopoietic progenitor cells[2]. At a concentration of 2.5 μM, BIBR 1532 diminishes colony-forming ability, induces telomere shortening, and sensitizes cells to chemotherapy by inhibiting telomerase activity in both MCF-7/WT and MCF-7/MlnR cell lines resistant to melphalan[3]. BIBR 1532 exhibits dose-dependent cytotoxicity in T-cell prolymphocytic leukemia (T-PLL)[4]. When combined with carboplatin, BIBR 1532 eradicates spheroid-forming ovarian cancer cells in ES2, SKOV3, and TOV112D cell lines[5]. |
体外研究 | BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay[1]. BIBR 1532 inhibits telomerase activity in a non-competitive manner[1]. BIBR 1532 reduces the proliferation of JVM13 leukemia cells, achieving an IC50 of 52 μM, a similar inhibition observed in other leukemia lines like Nalm-1, HL-60, and Jurkat. BIBR 1532's antiproliferative effects on acute myeloid leukemia (AML) are noted with an IC50 of 56 μM, while it does not affect the proliferative ability of normal hematopoietic progenitor cells[2]. At a concentration of 2.5 μM, BIBR 1532 diminishes colony-forming ability, induces telomere shortening, and sensitizes cells to chemotherapy by inhibiting telomerase activity in both MCF-7/WT and MCF-7/MlnR cell lines resistant to melphalan[3]. BIBR 1532 exhibits dose-dependent cytotoxicity in T-cell prolymphocytic leukemia (T-PLL)[4]. When combined with carboplatin, BIBR 1532 eradicates spheroid-forming ovarian cancer cells in ES2, SKOV3, and TOV112D cell lines[5]. |
Concentration | Treated Time | Description | References | |
HeLa cells | 20 µM | 10 days | To investigate the effect of BIBR1532 on HeLa cell proliferation, the results showed that BIBR1532 significantly inhibited cell proliferation | Cell Death Dis. 2019 Jul 11;10(7):527. |
EBV-positive lymphoblastoid cell lines and Burkitt’s lymphoma cell lines | 30 µM | 16, 24, 36, 48 and 72 hours | To evaluate the effect of BIBR on cell proliferation and apoptosis. | Cell Death Dis. 2016 Dec 29;7(12):e2562. |
Primary mouse hepatocytes | 20 µM | 24 hours | To assess the effects on SASP expression and signaling pathways. | Cell Mol Life Sci. 2024 Apr 30;81(1):200. |
MCF-7 and MDA-MB 231 cells | 50 µM | 48 hours | The purpose was to assess apoptosis induction; results indicated a decrease in apoptotic cells when treated with BIBR 1532. | Cancer Cell Int. 2014 Jul 4;14:60. |
MCF-7 cells | 20 µM | To investigate the effect of BIBR1532 on MCF-7 cell proliferation, the results showed that BIBR1532 significantly inhibited cell proliferation | Cell Death Dis. 2019 Jul 11;10(7):527. |
Administration | Dosage | Frequency | Description | References | ||
Balb/c mice | 4T1 cell xenograft breast cancer model | IntratumOral injection | 10 mg/kg/d | Once daily for 14 days | To investigate the effect of BIBR1532 on 4T1 cell xenograft breast cancer model, the results showed that BIBR1532 significantly inhibited tumor growth | Cell Death Dis. 2019 Jul 11;10(7):527. |
Dose | Nude Mice: 1 mg/kg - 2 mg/kg[2] (i.p.) Mice: 100 mg/kg[3] (p.o.) |
Administration | i.p., p.o. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.02mL 0.60mL 0.30mL |
15.09mL 3.02mL 1.51mL |
30.18mL 6.04mL 3.02mL |
CAS号 | 321674-73-1 |
分子式 | C21H17NO3 |
分子量 | 331.36 |
SMILES Code | O=C(O)C1=CC=CC=C1NC(/C=C(C2=CC=C3C=CC=CC3=C2)\C)=O |
MDL No. | MFCD11112195 |
别名 | Telomerase Inhibitor X |
运输 | 蓝冰 |
InChI Key | PGFQXGLPJUCTOI-WYMLVPIESA-N |
Pubchem ID | 9927531 |
存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
溶解方案 |
DMSO: 105 mg/mL(316.87 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的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
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