1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase
  3. SP-146

SP-146 

Cat. No.: HY-131339
Handling Instructions

SP-146 is a  highly potent, selective and non-ATP-competitive Aurora B inhibitor with an IC50 of 0.316 nM, and shows >2000 fold selectivity against FLT3 (IC50=1475.6 nM) and KIT (IC50=1307.6 nM). SP-146 is not promiscuous, rather selective for a few cancer cells, incluing MDA-MD-468 (GI50=107 nM). SP-146 can be used for the research of triple negative breast cancer (TNBC).

For research use only. We do not sell to patients.

SP-146 Chemical Structure

SP-146 Chemical Structure

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Description

SP-146 is a  highly potent, selective and non-ATP-competitive Aurora B inhibitor with an IC50 of 0.316 nM, and shows >2000 fold selectivity against FLT3 (IC50=1475.6 nM) and KIT (IC50=1307.6 nM). SP-146 is not promiscuous, rather selective for a few cancer cells, incluing MDA-MD-468 (GI50=107 nM). SP-146 can be used for the research of triple negative breast cancer (TNBC)[1].

IC50 & Target[1]

Aurora A

0.316 nM (IC50)

Aurora B

18.975 nM (IC50)

In Vitro

SP-146 (0-1 µM; 24 hours) is not promiscuous, rather selective for a few cell lines, it inhibits MDA-MB-468, CCRF-CEM, COLO 205 and A498 cell growth with GI50 values of 107 nM,47.4 nM, 50.3 nM and 53.2 nM, respectively[1].
SP-146 (63.2 nM) inhibits Aurora B activity in H460 cells by the characteristics of increased DNA content, and it increases cell volume with enormous nucleus[1].
SP-146 (0-2 µM) inhibits Aurora B enzymatic activity with an IC50 of 0.316 nM and inhibits Aurora A with observed IC50 value of 18.975 nM. SP-146 shows >2000 fold selectivity against FLT3 (IC50=1475.6 nM) and KIT (IC50=1307.6 nM). Meanwhile, it exhibits inhibitory effects on other receptor tyrosine kinases (RTKs) namely EGFR, RET and HER2 with IC50 value ≥2 µM[1].

Cell Viability Assay[1]

Cell Line: MDA-MB-468, CCRF-CEM, COLO 205 and A498 cell
Concentration: 0-1 µM
Incubation Time: 24 hours
Result: Showed good activity on MDA-MB-468 cells.
Molecular Weight

453.47

Formula

C₂₅H₂₀FN₇O

SMILES

O=C(NC1=CC=CC(NC2=C3C=CC(C4=CN(C)N=C4)=CC3=NC=N2)=C1)NC5=CC=CC(F)=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

SP-146SP146SP 146Aurora KinasehematopoiesisNCI60MDA-MD-468Triple NegativeBreast Cancer,Inhibitorinhibitorinhibit

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