BIBR 1532

CAS号

321674-73-1

分子式

C21H17NO3

主要靶点

Telomerase|Apoptosis

仅限科研使用

Cat No : CM06609

Print datasheet

Synonyms

inhibit|Apoptosis|BIBR1532|BIBR-1532|BIBR 1532|Inhibitor|Telomerase



产品信息

CAS号 321674-73-1
分子式 C21H17NO3
主要靶点 Telomerase|Apoptosis
主要通路 DNA 损伤和修复|凋亡
分子量 331.36
纯度 99.36%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 inhibit|Apoptosis|BIBR1532|BIBR-1532|BIBR 1532|Inhibitor|Telomerase

靶点活性

Telomerase:100 nM

体内活性

在MCF-7/WT和抗美法仑的MCF-7/MlnR 细胞系中,BIBR 1532(2.5 μM)通过抑制端粒酶活性降低形成集落的能力,并缩短端粒长度,且诱导对化疗增敏。在体外,BIBR 1532剂量依赖性地非竞争性抑制端粒酶活性(IC50:100 nM)。BIBR 1532对T细胞幼淋巴细胞白血病具有选择性细胞毒性,该毒性具有剂量依赖性,BIBR 1532处理过的细胞也出现核浓缩及凋亡小体形成现象。在JVM13白血病细胞系中,BIBR 1532具有剂量依赖性的抗增殖效果(IC50:52 μM),且对其他白血病细胞系,包括 Nalm-1,HL-60和Jurkat的结果相似。此外, 在急性髓细胞性白血病中,BIBR 1532具有抗增殖效果(IC50:56 μM),而且不影响正常造血干细胞的增殖能力。

溶解度

DMSO:21.67 mg/mL (65.39 mM);Ethanol:8.3 mg/mL (25 mM)

细胞实验

Cells are plated as triplicates in complete RPMI 1640 medium with various concentrations of BIBR1532. After 24 to 72 hours, water-soluble tetrazolium (WST-1) is added, which is transformed into formazan by mitochondrial reductase systems. The increase in the number of viable cells results in an increase of activity of mitochondrial dehydrogenases, leading to an increase of formazan dye formed, which is quantified by ELISA reader after 2, 3, and 4 hours of incubation. (Only for Reference)

参考文献

1.Pascolo E, et al. J Biol Chem. 2002, 277(18), 15566-15572.
2.El-Daly H, et al. Blood. 2005, 105(4), 1742-1749.
3.Ward RJ, et al. Mol Pharmacol. 2005, 68(3), 779-786.
4.R?th A, et al. Leukemia. 2007, 21(12), 2456-2462.
5.Meng E, et al. Gynecol Oncol. 2012, 124(3), 598-605.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
=
×
×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
×
=
×
C1   V1   C2   V2