ANI-7

ANI-7是芳香烃受体(AhR)途径的激活剂。ANI-7抑制多种癌症细胞的生长,并有效且选择性地抑制MCF-7乳腺癌症细胞的生长(GI50:0.56μM)。

CAS号

931417-26-4

分子式

C13H8Cl2N2

主要靶点

Chk

仅限科研使用

Cat No : CM13103

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Synonyms



产品信息

ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells and potently and selectively inhibits the growth of MCF-7 breast cancer cells (GI50: 0.56 μM).

CAS号 931417-26-4
分子式 C13H8Cl2N2
主要靶点 Chk
主要通路 细胞周期
分子量 263.12
纯度 99.21%, 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
别名

体外活性

ANI-7 (2.5 μM; 24 hours; MCF10A and MDA-MB-468 cells) treatment induces significant S-phase and G2 + M-phase cell cycle arrest within 24 hours of treatment in MDA-MB-468 cells. ANI-7 (2 μM; 12-24 hours; MDA-MB-468 cells) treatment results in a significant increase in the content and phosphorylation of CHK2, and induces a significant increase in H2AXɣ in MDA-MB-468 cells, indicative of DNA double-strand damage. Comparisons of the GI50 values show that ANI-7 produces a GI50 value of 0.38 μM in MCF-7 cells, whereas values of 3.0-42 μM are observed in cell lines from lung, colon, ovary, neuronal, glial, prostate, and pancreas. The only other tumor type that shows appreciable growth inhibition by ANI-7 is the A431 vulva cell line (GI50 of 0.51μM). ANI-7 potently inhibits the growth of T47D, ZR-75-1, MCF-7, SKBR3, and MDA-MB-468 breast cancer cells (GI50 range of 0.16-0.38 μM), moderately inhibits the growth of BT20 and BT474 cells (GI50 range of 1-2 μM), and essentially fails to inhibit the growth of MDA-MB-231 and MCF10A cells (GI50 range of 17-26 μM). Moreover, ANI-7 maintained its ability to inhibit the growth of drug-resistant cells (MCF-7/VP16: GI50 of 0.21 μM) [1].

溶解度

DMSO:18.7 mg/mL (71.3 mM),Sonification is recommended.

参考文献

1.Gilbert J, et al. (Z)-2-(3,4-Dichlorophenyl)-3-(1H-Pyrrol-2-yl)Acrylonitrile Exhibits Selective Antitumor Activity in Breast Cancer Cell Lines via the Aryl Hydrocarbon Receptor Pathway. Mol Pharmacol. 2018 Feb;93(2):168-177.
2.Baker JR, et al. Dichlorophenylacrylonitriles as AhR Ligands That Display Selective Breast Cancer Cytotoxicity in vitro. ChemMedChem. 2018 Jul 18;13(14):1447-1458.
3.Mark Tarleton, et al. Library synthesis and cytotoxicity of a family of 2-phenylacrylonitriles and discovery of an estrogen dependent breast cancer lead compound.  Medicinal Chemistry Communication. January 20112. (1):31-37.

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