PLK1-IN-6 

PLK1-IN-6 is a potent and selective PLK1 inhibitor, with an IC₅₀ of 0.45 nM. PLK1-IN-6 shows significant anti-proliferative activities against cancer cells^[1].

PLK1-IN-6 (compound 21 g) shows significant anti-proliferative activities against four tumor-derived cell lines (MCF-7 IC₅₀=8.64 nM, HCT-116 IC₅₀=26.0 nM, MDA-MB-231 IC₅₀=14.8 nM and MV4-11 IC₅₀=47.4 nM)^[1].
PLK1-IN-6 shows moderate metabolism and the half-life in human liver microsome is 25.7 min^[1].

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

PLK1-IN-6 (compound 21 g) (1 mg/kg; i.v.) exhibits a good half-life (10.1 h) and area under plasma concentration curves in Sprague Dawley rats^[1].
PLK1-IN-6 (10 mg/kg; i.g.) exhibits low clearance values and high plasma exposure (26800 ng•h/mL), with favorable bioavailability (11.4%) in Sprague Dawley rats^[1].
PLK1-IN-6 (10 mg/kg; i.g.) exhibits long half-life (2.73 h), high plasma exposure (11227 ng•h/mL) and excellent bioavailability (77.4%) in Balb/c mice^[1].
PLK1-IN-6 (20 mg/kg; i.g.) shows no apparent toxicity in mice^[1].

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

547.65

C₂₈H₃₇N₉O₃

3038489-04-9

CC[C@@H]1C(N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C5=NOC(CN6CCNCC6)=N5)OC)C)=O

Room temperature in continental US; may vary elsewhere.

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

• [1]. Li Z, et, al. Design, synthesis, and biological evaluation of novel dihydropteridone derivatives possessing oxadiazoles moiety as potent inhibitors of PLK1. Eur J Med Chem. 2023 May 5;251:115242.  [Content Brief]