LY3295668

For research use only.

Catalog No.S8782 Synonyms: AK-01

1 publication

LY3295668 Chemical Structure

CAS No. 1919888-06-4

LY3295668 (AK-01) is a potent, orally active and specific inhibitor of Aurora A kinase with Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively.

Selleck's LY3295668 has been cited by 1 publication

Purity & Quality Control

Choose Selective Aurora Kinase Inhibitors

Biological Activity

Description LY3295668 (AK-01) is a potent, orally active and specific inhibitor of Aurora A kinase with Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively.
Targets
AURKA [1]
(Cell-free assay)
0.8 nM(Ki)
In vitro

LY3295668, an AURKA inhibitor with over 1,000-fold selectivity versus AURKB, is distinguished by minimal toxicity to bone marrow cells at concentrations active against RB1mut cancer cells.[1]

In vivo

LY3295668 leads to durable regression of RB1mut tumor xenografts at exposures that are well tolerated in rodents. Genetic suppression screens identifi ed enforcers of the spindle-assembly checkpoint (SAC) as essential for LY3295668 cytotoxicity in RB1-defi cient cancers and suggest a model in which a primed SAC creates a unique dependency on AURKA for mitotic exit and survival.[1]

Protocol

Cell Research:

[1]

- Collapse
  • Cell lines: NCI-H446 cells, Calu-6 cells
  • Concentrations: 0.001 μM - 1 μM
  • Incubation Time: 24 h, 48 h, 72 h
  • Method:

    To measure apoptosis by IncuCyte Zoom instrument, NCI-H446 and Calu-6 cells are plated on Costar 3596 plates and treated with LY3295668 at different concentrations for 24, 48, and 72 hours. Caspase 3/7 activation is measured with Cell- Player 96-Well Kinetic Caspase 3/7 reagent. Green fluorescent images are acquired every 2 hours. Green objects counted (y-axis) are plotted against either real time (x-axis) or raw numbers as percent control.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: 7–8 week-old athymic nude female mice
  • Dosages: 50 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 98 mg/mL (200.02 mM)
Water Insoluble
Ethanol ''''15 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 489.95
Formula

C24H26ClF2N5O2

CAS No. 1919888-06-4
Storage powder
in solvent
Synonyms AK-01
Smiles CC1CC(CCN1CC2=C(C(=CC=C2)Cl)F)(CC3=C(C=CC(=N3)NC4=NNC(=C4)C)F)C(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03898791 Completed Drug: LY3295668 Erbumine Small Cell Lung Cancer Eli Lilly and Company July 16 2019 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Aurora Kinase Signaling Pathway Map

Related Aurora Kinase Products

Tags: buy LY3295668 | LY3295668 supplier | purchase LY3295668 | LY3295668 cost | LY3295668 manufacturer | order LY3295668 | LY3295668 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID