LY3295668 erbumine
Based on 3 publication(s) in Google Scholar
LY3295668 (AK-01) erbumine is a highly specific and orally active inhibitor of Aurora-A kinase with a Ki values for AurA and AurB of 0.8 nM and 1038 nM respectively. LY3295668 erbumine can effectively inhibit the autophosphorylation of AurA, induce mitotic arrest and apoptosis. LY3295668 erbumine avoids the formation of polyploids related to AurB inhibition. LY3295668 erbumine can be used for the study of small cell lung cancer.
For research use only. We do not sell to patients.
- CAS No.: 1919888-07-5
- Formula: C28H37ClF2N6O2
- Molecular Weight:563.08
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) LY3295668 erbumine
MoreAll Aurora Kinase Isoforms
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Biological Activity
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Aurora A 0.8 nM (Ki) |
Aurora B 1038 nM (Ki) |
Chemical Information
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CAS No. 1919888-07-5
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Molecular Weight 563.08
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Formula C28H37ClF2N6O2
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SMILES
CC(C)(N)C.OC([C@]1(C[C@H](N(CC1)CC2=C(C(Cl)=CC=C2)F)C)CC3=C(F)C=CC(NC4=NNC(C)=C4)=N3)=O
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Synonyms
AK-01 erbumine
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Anti-tumor efficacy of HRS-4642 and its potential combination with proteasome inhibition in KRAS G12D-mutant cancer. [Abstract]2024 Jul 8;42(7):1286-1300.e8. PMID: 38942026 -
J Med Chem
Second-Generation AURKA-Targeting PROTACs: Structural Optimization toward in Vivo Degradation in Neuroblastoma. [Abstract]2025 Nov 27;68(22):23962-23976. PMID: 41252673 -
Invest New Drugs
TAS-119, a novel selective Aurora A and TRK inhibitor, exhibits antitumor efficacy in preclinical models with deregulated activation of the Myc, β-Catenin, and TRK pathways. [Abstract]2021 Jun;39(3):724-735. PMID: 33409897
Purity & Documentation
References
[1]. Gong X, et al. Aurora-A kinase inhibition is synthetic lethal with loss of the RB1 tumor suppressor gene. Cancer Discov. 2018 Oct 29. pii: CD-18-0469. [Content Brief]
[2]. Du J, et al. Aurora A-Selective Inhibitor LY3295668 Leads to Dominant Mitotic Arrest, Apoptosis in Cancer Cells, and Shows Potent Preclinical Antitumor Efficacy. Mol Cancer Ther. 2019 Dec;18(12):2207-2219. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LY3295668 erbumine Related Classifications
HY-114258A Related Classifications
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