ANI-7

CAS号

931417-26-4

分子式

C13H8Cl2N2

主要靶点

Chk

仅限科研使用

Cat No : CM13103

Print datasheet

Synonyms

Chk2|ANI 7|ANI7|ANI-7



产品信息

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 | Shipping with blue ice.
别名 Chk2|ANI 7|ANI7|ANI-7

体外活性

ANI-7 (2.5 μM; 24小时; MCF10A和MDA-MB-468细胞)处理在MDA-MB-468细胞中24小时内显著诱导S期和G2 + M期的细胞周期阻滞。ANI-7 (2 μM; 12-24小时; MDA-MB-468细胞)处理显著增加CHK2的含量和磷酸化,使MDA-MB-468细胞中H2AX?显著增加,表明双链DNA损伤。GI50值比较显示,ANI-7在MCF-7细胞中产生0.38 μM的GI50值,而在肺、结肠、卵巢、神经元、神经胶质、前列腺和胰腺的细胞系中观察到3.0-42 μM的值。A431外阴细胞系是唯一一个由ANI-7显著抑制生长的其他肿瘤类型(GI50为0.51μM)。ANI-7强效抑制T47D、ZR-75-1、MCF-7、SKBR3和MDA-MB-468乳腺癌细胞的生长(GI50范围0.16-0.38 μM),适度抑制BT20和BT474细胞的生长(GI50范围1-2 μM),并且实际上未能抑制MDA-MB-231和MCF10A细胞的生长(GI50范围17-26 μM)。此外,ANI-7保持了抑制耐药细胞生长的能力(MCF-7/VP16: GI50为0.21 μM)[1]。

溶解度

DMSO:45 mg/mL (171.02 mM)

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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