ON1231320 | GBO-006 | CAS#1312471-39-8 | PLK2 inhibitor

MedKoo Cat#: 206799 | Name: ON1231320

Description:

WARNING: This product is for research use only, not for human or veterinary use.

ON1231320, also known as GBO-006, is a Polo-like kinase 2 (PLK2) inhibitor. In vitro testing revealed that ON1231320 is a selective inhibitor of PLK2 with no inhibitory activity against PLK1, PLK3 and PLK4. The cytotoxic effect of the drug is mediated by apoptosis as evidenced by the induction of Caspase 3/7 activity and by the cleavage of PARP in a dose dependent manner. ON1231320 affects cell cycle progression by blocking tumor cells in the G2/M phase however it does not affect normal human fibroblasts.

Chemical Structure

ON1231320

CAS#1312471-39-8

Theoretical Analysis

MedKoo Cat#: 206799

Name: ON1231320

CAS#: 1312471-39-8

Chemical Formula: C22H15F2N5O3S

Exact Mass: 467.0864

Molecular Weight: 467.45

Elemental Analysis: C, 56.53; H, 3.23; F, 8.13; N, 14.98; O, 10.27; S, 6.86

Price and Availability

Size	Price	Availability
50mg	USD 550.00	2 Weeks
100mg	USD 950.00	2 Weeks
200mg	USD 1,650.00	2 Weeks
500mg	USD 2,450.00	2 Weeks
1g	USD 3,650.00	2 Weeks
2g	USD 5,850.00	2 Weeks
5g	USD 8,650.00	2 Weeks

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Synonym

ON1231320; ON-1231320; ON 1231320; GBO-006; GBO006; GBO 006.

IUPAC/Chemical Name

2-((1H-indol-5-yl)amino)-6-((2,4-difluorophenyl)sulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one

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 Code

C1=CC(F)=CC(F)=C1S(=O)(=O)C1=CC2=CN=C(NC3=CC=C4NC=CC4=C3)N=C2N(C)C1=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

The Polo like kinases play key roles in mitosis. While the upregulation of PLK1 in cancer is well documented and PLK3 has been demonstrated to be a tumor suppressor, little is known about the oncogenic significance of PLK2. PLK2 kinase activity is essential for centriolar duplication and is also believed to play a regulatory role in the survival pathway by physically stabilizing the TSC1/2 complex in tumor cells under hypoxic conditions. Protein tyrosine hyper-phosphorylation and the upregulation of serine/threonine kinases associated with cell cycle progression have been linked to the etiology of cancer.

Product Data

Product Data

Instruction

View handling instruction

Biological target:

ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC50 of 0.31 µM.

In vitro activity:

ON1231320 dampened the growth of human glioma cells. The data illustrated that inoculation with 200 nm ON1231320 caused remarkable glioma cell growth dampening at 24, 48 h and 72 h (Figure 8A). Meanwhile ON1231320 promoted cleaved PARP expression and dampened the expression of PLK2 in a dose-dependent approach. These data suggest that ON1231320 shows its antitumor properties in glioma cells. Reference: Aging (Albany NY). 2022 Mar 7;14(5):2320-2334. https://pubmed.ncbi.nlm.nih.gov/35256538/

In vivo activity:

To determine the efficacy of compound 7ao in vivo using a tumor xenograft model, MDAMB-231 triple negative breast cancer cells were injected subcutaneously into nude mice. Once the tumors reached an average volume of 70 mm3, 7ao was administered on alternate days (Q2D) via intraperitoneal (IP) injection at a dose of 75 mg/kg body weight. This treatment with 7ao resulted in significant inhibition of tumor growth (86.5%) as compared to the control group (Fig. 6A), and no overt signs of toxicity were observed in the 7ao treated group (body weights shown in Fig. 6B). Reference: Bioorg Med Chem. 2016 Feb 15;24(4):521-44. https://pubmed.ncbi.nlm.nih.gov/26762835/

	Solvent	mg/mL	mM
Solubility
	DMSO	35.5	75.94

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 467.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Ding Y, Liu H, Zhang C, Bao Z, Yu S. Polo-like kinases as potential targets and PLK2 as a novel biomarker for the prognosis of human glioblastoma. Aging (Albany NY). 2022 Mar 7;14(5):2320-2334. doi: 10.18632/aging.203940. Epub 2022 Mar 7. PMID: 35256538; PMCID: PMC8954957. 2. Reddy MV, Akula B, Jatiani S, Vasquez-Del Carpio R, Billa VK, Mallireddigari MR, Cosenza SC, Venkata Subbaiah DR, Bharathi EV, Pallela VR, Ramkumar P, Jain R, Aggarwal AK, Reddy EP. Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2). Bioorg Med Chem. 2016 Feb 15;24(4):521-44. doi: 10.1016/j.bmc.2015.11.045. Epub 2015 Dec 1. PMID: 26762835; PMCID: PMC5947326.

In vitro protocol:

In vivo protocol:

1: Ding Y, Liu H, Zhang C, Bao Z, Yu S. Polo-like kinases as potential targets and PLK2 as a novel biomarker for the prognosis of human glioblastoma. Aging (Albany NY). 2022 Mar 7;14(5):2320-2334. doi: 10.18632/aging.203940. Epub 2022 Mar 7. PMID: 35256538; PMCID: PMC8954957. 2: Cashman R, Haim-Abadi G, Lezmi E, Philip H, Nissenbaum J, Viner-Breuer R, Kozulin C, Golan-Lev T, Gadban A, Spinner-Potesky S, Yanuka O, Kopper O, Benvenisty N. Genome-Wide Screening in Haploid Stem Cells Reveals Synthetic Lethality Targeting MLH1 and TP53 Deficient Tumours. Cell Prolif. 2025 Jan 15:e13788. doi: 10.1111/cpr.13788. Epub ahead of print. PMID: 39814695.