ANI-7

小分子

ANI-7

A648810-5mg

5mg

≥98%

-20°C储存

超低温冰袋运输

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 with a GI 50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines 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 GI 50 values show that ANI-7 produces a GI 50 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 (GI 50 of 0.51μM) . ANI-7 potently inhibits the growth of T47D, ZR-75-1, MCF-7, SKBR3, and MDA-MB-468 breast cancer cells (GI 50 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 (GI 50 range of 17-26 μM). Moreover, ANI-7 maintained its ability to inhibit the growth of drug-resistant cells (MCF-7/VP16: GI 50 of 0.21 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell 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 AnalysisCell 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 H2AXɣ (3.5-fold increase). Form:Solid IC50& Target:Aryl Hydrocarbon Receptor Chk2

ANI-7 是芳基烃受体（AhR）通路的激活剂。ANI-7 可抑制多种癌细胞的生长，对 MCF-7 乳腺癌细胞的生长具有强效的选择性抑制作用，其 GI 50 为 0.56 μM。ANI-7能诱导CYP1-代谢酶的活性。

931417-26-4

C13H8Cl2N2

263.12 g/mol

11565176

C1=CNC(=C1)/C=C(\C#N)/C2=CC(=C(C=C2)Cl)Cl

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

1S/C13H8Cl2N2/c14-12-4-3-9(7-13(12)15)10(8-16)6-11-2-1-5-17-11/h1-7,17H/b10-6+

IJJHHDLGGYDXGD-UXBLZVDNSA-N

C1=CNC(=C1)C=C(C#N)C2=CC(=C(C=C2)Cl)Cl

11565176

DMSO : 20.83 mg/mL (79.17 mM; Need ultrasonic)

1

1

2

262.006 Da

262.006 Da

39.600 Ų

17

0

345.000

0

1

3.800