| Size | Price | |
|---|---|---|
| 5mg | ||
| 10mg | ||
| 25mg | ||
| 50mg | ||
| 100mg | ||
| 250mg | ||
| 500mg | ||
| Other Sizes |
| Targets |
Polo-like kinase 2 (PLK2), IC50 = 0.31 μM. ON1231320 blocks tumor cell cycle progression in G2/M phase, leading to apoptotic cell death.
|
|---|---|
| ln Vitro |
For PLK1, PLK3, and PLK4 (all with IC50 values greater than 10 μM), ON1231320 (compound 7ao) exhibits no inhibitory effect [1]. Human tumor cells that have been exposed to ON1231320 (0–5 μM) for 24 hours undergo programmed cell death. Inhibiting 16 tumor cell lines (IC50=0.035-0.2 μM)[1], ON1231320 inhibits DU145, MCF-7, BT474, SK-OV-3, MIA-PaCa-2, SK-MEL-28, A549, U87, COLO -205, HELA, H1975, RAJI, U205, K562, GRANTA-519. [1] Tubulin polymerization is not markedly inhibited by ON1231320. [2] Normal human fibroblasts are not affected by ON1231320.
ON1231320 is a highly specific PLK2 inhibitor with IC50 = 0.31 μM. It blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. It is an aryl sulfonyl pyridopyrimidinone compound with potential anticancer activity against breast and other cancer cell lines. |
| ln Vivo |
Compound 7ao, injected intraperitoneally every other day (Q2D) for 20 days at a dose of 75 mg/kg, demonstrated a substantial inhibition of tumor growth [1].
In vivo activity data for ON1231320 are limited. As a highly specific PLK2 inhibitor, its in vivo efficacy would be evaluated in tumor xenograft models following standard protocols for kinase inhibitors, including assessment of tumor growth inhibition and cell cycle marker modulation. |
| Enzyme Assay |
PLK2 kinase assays use purified recombinant PLK2 and a specific peptide substrate in the presence of ATP and ON1231320 at increasing concentrations. Phosphorylation is detected by radiometric or fluorescence-based methods. IC50 values are determined from dose-response curves. Selectivity is assessed against other PLK family kinases.
|
| Cell Assay |
Apoptosis Analysis[1]
Cell Types: U2OS cells Tested Concentrations: 0-5 µM Incubation Duration: 24 hrs (hours) Experimental Results: Increased the activity of Caspases 3/7 in a dose-dependent manner. Induced apoptosis. Cancer cell lines (breast, colon, etc.) are cultured in standard media and treated with ON1231320 at various concentrations. Cell cycle distribution is analyzed by flow cytometry after propidium iodide staining. Apoptosis is assessed by Annexin V/PI staining and caspase-3/7 activity assays. Cell viability is measured by MTT or sulforhodamine B assays. |
| Animal Protocol |
Animal/Disease Models: 6-8 week old NCR nu/nu female mice with MDAMB-231 triple negative breast cancer cells[1]
Doses: 75 mg/kg Route of Administration: IP; alternate days (Q2D) for 20 days Experimental Results: Resulted in significant inhibition of tumor growth (86.5%) Animal studies use tumor xenograft models in immunodeficient mice. ON1231320 is formulated in DMSO-saline or appropriate vehicle and administered intraperitoneally or orally at doses determined by pharmacokinetic studies. Tumor growth inhibition and survival are assessed. Tumor tissue is analyzed for cell cycle arrest (flow cytometry) and apoptosis markers (TUNEL, cleaved caspase-3). |
| References |
| Exact Mass |
467.0864
|
|---|---|
| CAS # |
131247-39-8
|
| Related CAS # |
131247-39-8;
|
| Appearance |
Light yellow to green yellow solid powder
|
| InChi Key |
ZEHBZHZMQSHZFI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H15F2N5O3S/c1-29-20-13(9-19(21(29)30)33(31,32)18-5-2-14(23)10-16(18)24)11-26-22(28-20)27-15-3-4-17-12(8-15)6-7-25-17/h2-11,25H,1H3,(H,26,27,28) SMILES
|
| Chemical Name |
2-((1H-indol-5-yl)amino)-6-((2,4-difluorophenyl)sulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one
|
| Synonyms |
ON1231320 ON-1231320 ON 1231320 GBO-006 GBO006 GBO 006.
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
