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
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M.Wt
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503.98
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Formula
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C25H28ClF2N5O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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)-
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References
1. Guiqun Yang, et al. Cancer Res (2023) 83 (7_Supplement): 1645.
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