1. Immunology/Inflammation
    Cell Cycle/DNA Damage
  2. Aryl Hydrocarbon Receptor
    Checkpoint Kinase (Chk)
  3. ANI-7

ANI-7 

Cat. No.: HY-117102 Purity: 99.25%
Handling Instructions

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 GI50 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.

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ANI-7 Chemical Structure

ANI-7 Chemical Structure

CAS No. : 931417-26-4

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Description

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 GI50 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[1][2][3].

IC50 & Target[1]

Aryl Hydrocarbon Receptor

 

Chk2

 

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[1].
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[1].
Inhibition of the AhR pathway ameliorates the effects of ANI-7. ANI-7 activates XRE activity and expression of the AhR and CYP1 members[1].
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)[1][1].
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].

Cell Cycle Analysis[1]

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[1]

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 H2AXɣ (3.5-fold increase).
Molecular Weight

263.12

Formula

C₁₃H₈Cl₂N₂

CAS No.

931417-26-4

SMILES

ClC1=CC(/C(C#N)=C/C2=CC=CN2)=CC=C1Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8005 mL 19.0027 mL 38.0055 mL
5 mM 0.7601 mL 3.8005 mL 7.6011 mL
10 mM 0.3801 mL 1.9003 mL 3.8005 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.91 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.91 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

ANI-7ANI7ANI 7Aryl Hydrocarbon ReceptorCheckpoint Kinase (Chk)AhRBreastcancercyclearrestDNAdouble-stranddamageCYP1Inhibitorinhibitorinhibit

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ANI-7
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HY-117102
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