LY3295668( LY-329566 | LY 329566 | AK-01 )

Catalog No. M13011 CAS No. 1919888-06-4

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Product Name

LY3295668
Note

Research use only, not for human use.
Brief Description

LY3295668 (LY-3295668, AK-01) is a novel potent, highly selective, orally active Aurora-A kinase inhibitor with Ki of 0.8 nM, H446 AurA auto-P IC50 of 0.6 nM.
Description

LY3295668 (LY-3295668, AK-01) is a novel potent, highly selective, orally active Aurora-A kinase inhibitor with Ki of 0.8 nM, H446 AurA auto-P IC50 of 0.6 nM; displays >1000-fold selectivity over Aur-B, 5/386 kinases were potently inhibited by LY3295668 (<10 nM) and none of these kinases overlapped with targets of the other AurAi (MK5108, alisertib), and no inhibition of SYK; LY3295668 is cytotoxic to RB1 mutant cancer cancaer cells (NCI-H446 cell IC50=0.752 uM), causes durable regression of RB1mut tumor xenografts.Solid Tumors Phase 2 Clinical.
In Vitro

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In Vivo

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Synonyms

LY-329566 | LY 329566 | AK-01
Pathway

Cell Cycle/DNA Damage
Target

Aurora Kinase
Recptor

Aurora Kinase
Research Area

Cancer
Indication

Solid Tumors

CAS Number

1919888-06-4
Formula Weight

489.952
Molecular Formula

C24H26ClF2N5O2
Purity

>98% (HPLC)
Solubility

DMSO : 150 mg/mL 306.15 mM
SMILES

ClC1=CC=CC(CN2CC[C@](C(O)=O)(CC3=C(F)C=CC(NC4=NNC(C)=C4)=N3)C[C@H]2C)=C1F
Chemical Name

(2R,4R)-1-(3-chloro-2-fluorobenzyl)-4-((3-fluoro-6-((5-methyl-1H-pyrazol-3-yl)amino)pyridin-2-yl)methyl)-2-methylpiperidine-4-carboxylic acid

1. Gong X, et al. Cancer Discov. 2018 Oct 29. pii: CD-18-0469.

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