ANI-7,931417-26-4

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ANI-7

CAS No. : 931417-26-4

MCE 国际站：ANI-7

产品活性：ANI-7 是一种 AhR 途径的激活剂。ANI-7 抑制多种癌细胞的生长，并有选择地抑制 MCF-7 乳腺癌细胞的生长，GI₅₀ 为 0.56 μM。ANI-7 通过激活 AhR 途径诱导 CYP1 代谢单加氧酶，并在敏感的乳腺癌细胞系中诱导 DNA 损伤，检查点激酶 (Chk2) 激活，S 期细胞周期停滞和细胞死亡。

研究领域：Immunology/Inflammation  |  Cell Cycle/DNA Damage

作用靶点：Aryl Hydrocarbon Receptor  |  Checkpoint Kinase (Chk)

In Vitro: 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 H2AXɣ 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).

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