1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP
  3. AG14361

AG14361 

Cat. No.: HY-12032 Purity: 98.54%
Handling Instructions

AG14361 is a potent PARP-1 inhibitor, with a Ki of < 5 nM, and in permeabilized SW620 and intact SW620 cells, the IC50s are 29 nM and 14 nM, respectively.

For research use only. We do not sell to patients.

AG14361 Chemical Structure

AG14361 Chemical Structure

CAS No. : 328543-09-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 179 In-stock
Estimated Time of Arrival: December 31
5 mg USD 163 In-stock
Estimated Time of Arrival: December 31
10 mg USD 307 In-stock
Estimated Time of Arrival: December 31
50 mg USD 931 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1603 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

AG14361 is a potent PARP-1 inhibitor, with a Ki of < 5 nM, and in permeabilized SW620 and intact SW620 cells, the IC50s are 29 nM and 14 nM, respectively.

IC50 & Target[1]

PARP-1

0.5 nM (Ki)

In Vitro

AG14361 is a potent PARP-1 inhibitor, with a Ki of < 5 nM, and in permeabilized SW620 and intact SW620 cells, the IC50s are 29 nM and 14 nM, respectively. AG14361 inhibits the proliferation of human cancer cells, such as A549, LoVo, and SW620 cells, with GI50s of 14 μM, 11.2 μM and 20 μM, respectively. Furthermore, AG14361 in combination with NSC 362856 markedly reduces the GI50 value of NSC 362856 in LoVo and A549 cells, but does not exert such an effect in SW620 cells[1]. AG14361 suppresses breast cancer cells with IC50s of 17 μM and 25 μM for 92 J-wt-BRCA1 and 92 J-sh-BRCA1 cells, respectively. AG14361 induces caspase 3/7 activation and cell cycle abnormalities, and also inhibits NF-κB signaling[2]. AG14361 (0.4 μM) enhances the growth-inhibitory and cytotoxic effects of topoisomerase I poisons, with no obvious effect on the formation and reversal of cleavable complexes, and increases the persistence of camptothecin-induced DNA single-strand breaks[3].

In Vivo

AG14361 (5 and 15 mg/kg, i.p.) has no toxicity and does not inhibit the growth of tumor. However, AG14361 markedly enhances NSC 362856 activity against LoVo xenografts and delays tumor growth when combined with NSC 362856. AG14361 (15 mg/kg, i.p.) treatment before irradiation dramaticly increases the sensitivity to radiation therapy of mice bearing LoVo xenografts[1]. AG14361 (30 mg/kg) synergizes lestaurtinib activity on inhibiting breast cancer tumors in allografts[2].

Molecular Weight

320.39

Formula

C₁₉H₂₀N₄O

CAS No.

328543-09-5

SMILES

O=C1NCCN2C3=C1C=CC=C3N=C2C4=CC=C(C=C4)CN(C)C

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 : 25 mg/mL (78.03 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1212 mL 15.6060 mL 31.2120 mL
5 mM 0.6242 mL 3.1212 mL 6.2424 mL
10 mM 0.3121 mL 1.5606 mL 3.1212 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: ≥ 2.5 mg/mL (7.80 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

The activity of full-length recombinant human PARP-1 is measured in a reaction mixture containing 20 nM PARP-1, 500 μM NAD+ plus [32P]NAD+ (0.1-0.3 μCi per reaction mixture), and activated calf thymus DNA (10 μg/mL) at 25°C; the reaction is terminated after 4 minutes by adding ice-cold 10% (wt/vol) trichloroacetic acid. The reaction product [32P]ADP-ribose incorporated into acid-insoluble material is deposited onto Whatman GF/C glass fiber filters with a microfiltration apparatus and quantified with a PhosphorImager. Inhibition of PARP-1 activity by AG14361 at 0-600 nM is measured, and the Ki for AG14361 is calculated by nonlinear regression analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

Cell viability assay is performed using a luciferase-coupled ATP quantization assay of metabolically active cells in a 96-well plate and MTT. For MTT, 1 to 2 × 104 cells are plated per one well of a 24-well plate. Target drugs (AG14361) at various concentrations are dissolved in DMSO and then added to the cells in 10% fetal bovine serum-containing Dulbecco’s modified Eagle’s medium (DMEM), IC50 concentration of AG14361 are also added to each well. The final DMSO concentration is kept at 0.1% after the addition to medium. After 48 hr medium is removed and 0.3 mL of 0.1% MTT in phosphate-buffered saline (PBS) is added in each well. After incubation for 30 min in a 37°C CO2 incubator, MTT solution is removed and 0.8 mL of 2-propanol is added. After shaking for 30 min, OD560 is measured using a plate reader. Plating for each time point is done in triplicate[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

CD-1 nude mice bearing palpable, subcutaneous SW620 or LoVo xenografts are treated intraperitoneally with normal saline (control animals) or AG14361 (at 5 or 15 mg/kg) alone daily for 5 days (five mice per group). For drug combinations, AG14361 is administered intraperitoneally daily for 5 days immediately before administering the cytotoxic drug (NSC 362856 at 68 mg/kg orally or CPT-11 at 2.5 mg/kg intraperitoneally) or 30 minutes before applying 2 Gy of x-irradiation locally to the tumor daily for 5 days. Tumor volumes, determined from two-dimensional caliper measurements and the equation a2 × b/2 (where a is the width and b is the length of the tumor), are presented as median relative tumor volume (RTV). That is, RTV1 is the tumor volume on the initial day of treatment (day 0), and RTV4 is the tumor volume 4 times that on the initial day of treatment. Tumor growth delay is defined as the time to RTV4 in drug-treated or irradiated mice compared with the time to RTV4 in control (vehicle alone) mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

AG14361AG 14361AG-14361PARPpoly ADP ribose polymeraseInhibitorinhibitorinhibit

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