2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. Aurora Kinase Apoptosis
  4. LY3295668

LY3295668 (AK-01) 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 can effectively inhibit the autophosphorylation of AurA, induce mitotic arrest and apoptosis. LY3295668 avoids the formation of polyploids related to AurB inhibition. LY3295668 can be used for the study of small cell lung cancer.

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LY3295668

LY3295668 Chemical Structure

CAS No. : 1919888-06-4

Size Prix Stock Quantité
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
1 mg En stock
5 mg En stock
10 mg En stock
25 mg En stock
50 mg En stock
100 mg En stock
200 mg   Obtenir un devis  
500 mg   Obtenir un devis  

* Veuillez sélectionner la quantité avant d'ajouter des articles.

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Based on 3 publication(s) in Google Scholar

Other Forms of LY3295668:

LY3295668 Related Antibodies

Top Publications Citing Use of Products

Voir tous les produits spécifiques à Isoform Aurora Kinase:

Voir toutes les isoformes
Aurora Kinase Aurora A Aurora B Aurora C

  • Activité biologique

  • Pureté et documentation

  • Références

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Description

LY3295668 (AK-01) 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 can effectively inhibit the autophosphorylation of AurA, induce mitotic arrest and apoptosis. LY3295668 avoids the formation of polyploids related to AurB inhibition. LY3295668 can be used for the study of small cell lung cancer[1][2].

IC50 & Target[1]

Aurora A

0.8 nM (Ki)

Aurora B

1038 nM (Ki)

In Vitro

LY3295668 is a highly specific Aurora-A kinase inhibitor, with Ki values of 0.8 nM and 1038 nM for AurA and AurB, respectively. LY3295668, a highly specific AurA inhibitor, can kill Rb-deficient cancer cells at doses that have minimal effects on normal cells. In a kinome-wide survey, only 5 of 386 kinases are potently inhibited by LY3295668 (<10 nM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

LY3295668 Related Antibodies
Essai clinique
Masse moléculaire

489.95

Formule

C24H26ClF2N5O2
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C([C@@]1(CC2=NC(NC3=NNC(C)=C3)=CC=C2F)C[C@@H](C)N(CC4=CC=CC(Cl)=C4F)CC1)O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvant et solubilité
In Vitro: 

DMSO : 80 mg/mL (163.28 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0410 mL 10.2051 mL 20.4102 mL
5 mM 0.4082 mL 2.0410 mL 4.0820 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation

Purity: 99.76%

SDS (252 KB)

COA (258 KB) HNMR (146 KB) RP-HPLC (171 KB) LCMS (105 KB)

Instruction de manipulation (2659 KB)
Références

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0410 mL 10.2051 mL 20.4102 mL 51.0256 mL
5 mM 0.4082 mL 2.0410 mL 4.0820 mL 10.2051 mL
10 mM 0.2041 mL 1.0205 mL 2.0410 mL 5.1026 mL
15 mM 0.1361 mL 0.6803 mL 1.3607 mL 3.4017 mL
20 mM 0.1021 mL 0.5103 mL 1.0205 mL 2.5513 mL
25 mM 0.0816 mL 0.4082 mL 0.8164 mL 2.0410 mL
30 mM 0.0680 mL 0.3402 mL 0.6803 mL 1.7009 mL
40 mM 0.0510 mL 0.2551 mL 0.5103 mL 1.2756 mL
50 mM 0.0408 mL 0.2041 mL 0.4082 mL 1.0205 mL
60 mM 0.0340 mL 0.1701 mL 0.3402 mL 0.8504 mL
80 mM 0.0255 mL 0.1276 mL 0.2551 mL 0.6378 mL
100 mM 0.0204 mL 0.1021 mL 0.2041 mL 0.5103 mL
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LY3295668 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LY32956681919888-06-4AK-01LY 3295668LY-3295668AK01AK 01Aurora KinaseApoptosisInhibitorinhibitorinhibit

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