Name: Poloppin
Brand: SIGMA

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About This Item

经验公式（希尔记法）:

C₂₀H₁₅BrF₃NO₂

CAS Number:

683808-78-8

分子量:

438.24

UNSPSC代码:

12352200

NACRES:

NA.77

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方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

2-8°C

SMILES字符串

OC(CCC1=CC=C(C2=CC=C(Br)C=C2)N1C3=CC=CC=C3C(F)(F)F)=O

InChI

1S/C20H15BrF3NO2/c21-14-7-5-13(6-8-14)17-11-9-15(10-12-19(26)27)25(17)18-4-2-1-3-16(18)20(22,23)24/h1-9,11H,10,12H2,(H,26,27)

InChI key

OCUKOJUZSNFVFQ-UHFFFAOYSA-N

生化/生理作用

Poloppin is a cell penetrant and potent inhibitor of mitotic Polo-like kinases (PLKs) that binds to the Polo-box domain (PBD) and prevents PLKs interaction with pSer/pThr phosphopeptide substrates. Poloppin induces mitotic arrest and apoptosis in cancer cells expressing mutant KRAS in 2D and organoid cultures. It also sensitizes mutant KRAS-expressing cancer cells to Crizotinib.

cell penetrant and potent inhibitor of PLKs that binds to the Polo-box domain (PBD) and prevents PLKs interaction with phosphopeptide substrates