|(4,4',5,5'-四氯-1'H-[1,3'-联吡咯] -2,2'-二基)双((2-羟苯基)甲酮)|CsnPharm

CAS No.: 1227962-62-0

(4,4',5,5'-Tetrachloro-1'H-[1,3'-bipyrrole]-2,2'-diyl)bis((2-hydroxyphenyl)methanone) Catalog No. CSN17591

Synonyms: Marinopyrrole A;(±)-Marinopyrrole A

Marinopyrrole A is a selective Mcl-1 inhibitor with IC50 of 10.1 μM and proapoptosis properties in some cancer cells.

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生物活性

实验方案

技术信息

生物活性

描述Maritoclax is a selective Mcl-1 inhibitor with IC50 value of 10.1μM against the binding of a biotinylated Bim BH3 peptide to Mcl-1 protein, but with IC50 value>80μM for Bcl-X_L. Maritoclax induced cell death with EC50 value of 1.6μM in K562 cells retrovirally transduced Mcl-1-IRES-BimEL and also exhibited anti-proliferation against primary large-granular lymphocyte leukemia (LGLL) cells with EC50 values ranging in 4.64-40μM correlated to the Mcl-1 level. Maritoclax at dose ranging in 1.5-2.5μM induced proteasome-mediated Mcl-1 degradation in Mcl-1-IRES-BimEL K562 cells at 12h post treatment, without induction of Mcl-1 phosphorylation and Noxa expression. Maritoclax, at concentration of 2 or 2.5μM, synergistically sensitized lymphoma/leukemia K562 cells and Raji cells to ABT-737, respectively, at 24h post treatment^[1]. Also Maritoclax could exhibited cytotoxicity in Mcl-1-independent manner in cells such as RS4;11 human leukemia cell line which have previously been shown to be dependent on Bcl-2 for survival^[2].
作用机制Maritoclax blocks the binding of Bim BH3 α-helix to Mcl-1 and induces Mcl-1 degradation, thereby leading to Mcl-1-dependent apoptosis.^[1]
动物研究
剂量
Nude Mice^[3] (i.p.): 20 mg/kg

给药途径
i.p.
参考文献

动物研究
剂量	Nude Mice^[3] (i.p.): 20 mg/kg
给药途径	i.p.

[1] Doi K, Li R, et al. Discovery of marinopyrrole A (maritoclax) as a selective Mcl-1 antagonist that overcomes ABT-737 resistance by binding to and targeting Mcl-1 for proteasomal degradation. J Biol Chem. 2012 Mar 23;287(13):10224-35.
[2] Eichhorn JM, Alford SE, et al. Purported Mcl-1 inhibitor marinopyrrole A fails to show selective cytotoxicity for Mcl-1-dependent cell lines. Cell Death Dis. 2013 Oct 24;4:e880.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9602 mL
- 9.8010 mL
- 19.6019 mL
- 5 mM
- 0.3920 mL
- 1.9602 mL
- 3.9204 mL
- 10 mM
- 0.1960 mL
- 0.9801 mL
- 1.9602 mL

技术信息

CAS号

1227962-62-0

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H12Cl4N2O4

运输

蓝冰

分子量

510.15

别名

Marinopyrrole A;(±)-Marinopyrrole A

溶解度

DMSO	160.0 mg/mL (313.6 mM)
Water	280.0 mg/mL (548.9 mM)

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(4,4',5,5'-Tetrachloro-1'H-[1,3'-bipyrrole]-2,2'-diyl)bis((2-hydroxyphenyl)methanone) Catalog No. CSN17591

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