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JAB-2485

Chemical Structure : JAB-2485

CAS No.: 2899209-55-1

JAB-2485 (JAB2485)

Catalog No.: PC-22152Not For Human Use, Lab Use Only.

JAB-2485 is a potent, highly selective small-molecule Aurora kinase A (AURKA) inhibitor with IC50 of 0.33 nM, with >1500-fold selectivity over AURKB and AURKC.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

JAB-2485 is a potent, highly selective small-molecule Aurora kinase A (AURKA) inhibitor with IC50 of 0.33 nM, with >1500-fold selectivity over AURKB and AURKC.
JAB-2485 significantly decreases the level of AURKA phosphorylation in a dose-dependent manner.
JAB-2485 induces cell cycle arrest and apoptosis in NCI-H446 cells, with minimal myelosuppression.
JAB-2485 inhibits in vitro proliferation of small cell lung cancer (SCLC), triple-negative breast cancer (TNBC) and neuroblastoma cell lines ( NCI-H2171, IC50=46.1 nM; SH-SY5Y IC50=8.1 nM).
JAB-2485 (10 mpk, p.o. QD) significantly inhibited in vivo tumor growth on MDA-MB-231 xenografts.

Physicochemical Properties

M.Wt 503.98
Formula C25H28ClF2N5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-Piperidinecarboxylic acid, 1-[(3-chloro-2-fluorophenyl)methyl]-4-[[5-fluoro-4-methyl-6-[(3-methyl-1H-pyrazol-5-yl)amino]-2-pyridinyl]methyl]-2-methyl-, (2R,4R)-

References

1. Guiqun Yang, et al. Cancer Res (2023) 83 (7_Supplement): 1645.

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