ON1231320
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MedKoo CAT#: 206799

CAS#: 1312471-39-8

Description: 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

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ON1231320
CAS# 1312471-39-8
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 206799
Name: ON1231320
CAS#: 1312471-39-8
Chemical Formula: C22H15F2N5O3S
Exact Mass: 467.09
Molecular Weight: 467.451
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 Quantity
50mg USD 550 2 Weeks
100mg USD 950 2 Weeks
200mg USD 1650
500mg USD 2450
1g USD 3650 2 Weeks
2g USD 5850
5g USD 8650
Bulk inquiry

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:
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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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 35.5 75.94

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.

Recalculate based on batch purity %
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: 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 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. 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.

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http://cancerres.aacrjournals.org/content/71/8_Supplement/643