LY3295668

Research use only, not for human use.

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.

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.

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LY-329566 | LY 329566 | AK-01

Cell Cycle/DNA Damage

Aurora Kinase

Aurora Kinase

Cancer

Solid Tumors

1919888-06-4

489.952

C24H26ClF2N5O2

>98% (HPLC)

DMSO : 150 mg/mL 306.15 mM

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

(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

(-20℃)

With Ice Pack

≥ 2 years