ANI-7

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的（高达 263 倍）乳腺癌细胞抑制剂，通过激活芳基烃受体 (AhR) 途径，GI50 为 0.5 uM (MCF-7)。

A potent and selective (up to 263-fold) inhibitor of breast cancer cells with GI50 of 0.5 uM (MCF-7), via activation the aryl hydrocarbon receptor (AhR) pathway; inhibits other cell lines derived from other tumour types with GI50 of 3.2-46 uM (lung, colon, ovary, neuronal, glial, prostate, and pancreas); potently inhibits the growth of T47D, ZR-75-1, MCF-7, SKBR3, and MDA-MB-468 breast cancer cells with GI50 of 0.16-0.38 uM, induces cell cycle arrest checkpoint activation and DNA damage; binds to the AhR, induces translocation to the nucleus, activates the XRE, induces CYP1 activity, culminating in cell cycle arrest, checkpoint activation, DNA damage and cell death.

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, and negligible effect in normal breast MCF10A 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 H2AX? in MDA-MB-468 cells, indicative of DNA double-strand damage.Inhibition of the AhR pathway ameliorates the effects of ANI-7. ANI-7 activates XRE activity and expression of the AhR and CYP1 members.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). Cell Cycle Analysis Cell Line:MCF10A and MDA-MB-468 cells Concentration:2.5 μM Incubation Time:24 hours Result:Induced significant S-phase and G2 + M-phase cell cycle arrest in MDA-MB-468 cells, and negligible effect in normal breast MCF10A cells.Western Blot Analysis Cell Line:MDA-MB-468 cells Concentration:2 μM Incubation Time:12 hours, 24 hours Result:Resulted in a significant increase in the content and phosphorylation of CHK2 (25-fold increase),and induced a significant increase in H2AX? (3.5-fold increase).

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ANI 7 | ANI7

Endocrinology/Hormones

AhR

AhR

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931417-26-4

263.121

C13H8Cl2N2

>98% (HPLC)

In Vitro:?DMSO : 20.83 mg/mL (79.17 mM)

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(Z)-2-(3,4-dichlorophenyl)-3-(1H-pyrrol-2-yl)acrylonitrile

(-20℃)

With Ice Pack

≥ 2 years