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.
Product information
CAS Number: 1312471-39-8
Molecular Weight: 467.45
Formula: C22H15F2N5O3S
Chemical Name: 6-(2,4-difluorobenzenesulfonyl)-2-[(1H-indol-5-yl)amino]-8-methyl-7H,8H-pyrido[2,3-d]pyrimidin-7-one
Smiles: CN1C2=NC(NC3C=C4C=CNC4=CC=3)=NC=C2C=C(C1=O)S(=O)(=O)C1=CC=C(F)C=C1F
InChiKey: ZEHBZHZMQSHZFI-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 25 mg/mL (53.48 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
ON1231320 (Compound 7ao) has no inhibitory activity against PLK1, PLK3 and PLK4 (all IC50>10 µM). ON1231320 (0-5 µM; 24 hours) activates programmed cell death in human tumor cells. 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). ON1231320 does not appreciably inhibit tubulin polymerization. ON1231320 does not affect normal human fibroblasts.
In Vivo:
ON1231320 (Compound 7ao; 75 mg/kg; IP; alternate days (Q2D) for 20 days) results in significant inhibition of tumor growth.
Products are for research use only. Not for human use.
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