1. Cell Cycle/DNA Damage
    Apoptosis
  2. Polo-like Kinase (PLK)
    Apoptosis
  3. ON1231320

ON1231320 

Cat. No.: HY-100789
Handling Instructions

ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC50 of 0.31 µM. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity.

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

ON1231320 Chemical Structure

ON1231320 Chemical Structure

CAS No. : 1312471-39-8

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Description

ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC50 of 0.31 µM. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity[1][2].

IC50 & Target[1]

PLK2

0.31 μM (IC50)

PLK1

>10 μM (IC50)

PLK3

>10 μM (IC50)

PLK4

>10 μM (IC50)

In Vitro

ON1231320 (Compound 7ao) has no inhibitory activity against PLK1, PLK3 and PLK4 (all IC50>10 µM)[1].
ON1231320 (0-5 µM; 24 hours) activates programmed cell death in human tumor cells[1].
ON1231320 inhibits cell proliferation in 16 tumor cell lines (DU145, MCF-7, BT474, SK-OV-3, MIA-PaCa-2, SK-MEL-28, A549, U87, COLO-205, HELA, H1975, RAJI, U205, K562, GRANTA-519; IC50= 0.035-0.2 µM)[1].
ON1231320 does not appreciably inhibit tubulin polymerization[1]. ON1231320 does not affect normal human fibroblasts[2].

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

Apoptosis Analysis[1]

Cell Line: U2OS cells
Concentration: 0-5 µM
Incubation Time: 24 hours
Result: Increased the activity of Caspases 3/7 in a dose-dependent manner.
Induced apoptosis.
In Vivo

ON1231320 (Compound 7ao; 75 mg/kg; IP; alternate days (Q2D) for 20 days) results in significant inhibition of tumor growth[1].

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

Animal Model: 6-8 week old NCR nu/nu female mice with MDAMB-231 triple negative breast cancer cells[1]
Dosage: 75 mg/kg
Administration: IP; alternate days (Q2D) for 20 days
Result: Resulted in significant inhibition of tumor growth (86.5%)
Molecular Weight

467.45

Formula

C₂₂H₁₅F₂N₅O₃S

CAS No.
SMILES

O=C1C(S(=O)(C2=CC=C(F)C=C2F)=O)=CC3=CN=C(NC4=CC5=C(NC=C5)C=C4)N=C3N1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (53.48 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1393 mL 10.6963 mL 21.3927 mL
5 mM 0.4279 mL 2.1393 mL 4.2785 mL
10 mM 0.2139 mL 1.0696 mL 2.1393 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: 2.5 mg/mL (5.35 mM); Suspended solution; Need ultrasonic

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

ON1231320ON 1231320ON-1231320Polo-like Kinase (PLK)ApoptosisG2/MphasemitosisfibroblastsU2OSMDAMB-231triplenegativebreastInhibitorinhibitorinhibit

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ON1231320
Cat. No.:
HY-100789
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