LY3295668 erbumine
Based on 4 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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 98.79%
- CAS No.: 1919888-07-5
- Formule: C28H37ClF2N6O2
- Masse moléculaire:563.08
-
Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) LY3295668 erbumine
MoreVoir tous les produits spécifiques à Isoform Aurora Kinase
More
Activité biologique
Description
IC50 & Target
[1]|
Aurora A 0.8 nM (Ki) |
Aurora B 1038 nM (Ki) |
Chemical Information
-
CAS No. 1919888-07-5
-
Appearance Solid
-
Masse moléculaire 563.08
-
Formule C28H37ClF2N6O2
-
Color White to off-white
-
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
-
Synonyms
AK-01 erbumine
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
-
Journal Impact Factor
-
Most Recent
-
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
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (177.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.44 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.44 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 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 (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
-
Fiche technique (279 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Instruction de manipulation (2659 KB)
Références
[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]
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 (sealed storage, away from moisture). 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 | 1.7759 mL | 8.8797 mL | 17.7595 mL | 44.3987 mL |
| 5 mM | 0.3552 mL | 1.7759 mL | 3.5519 mL | 8.8797 mL | |
| 10 mM | 0.1776 mL | 0.8880 mL | 1.7759 mL | 4.4399 mL | |
| 15 mM | 0.1184 mL | 0.5920 mL | 1.1840 mL | 2.9599 mL | |
| 20 mM | 0.0888 mL | 0.4440 mL | 0.8880 mL | 2.2199 mL | |
| 25 mM | 0.0710 mL | 0.3552 mL | 0.7104 mL | 1.7759 mL | |
| 30 mM | 0.0592 mL | 0.2960 mL | 0.5920 mL | 1.4800 mL | |
| 40 mM | 0.0444 mL | 0.2220 mL | 0.4440 mL | 1.1100 mL | |
| 50 mM | 0.0355 mL | 0.1776 mL | 0.3552 mL | 0.8880 mL | |
| 60 mM | 0.0296 mL | 0.1480 mL | 0.2960 mL | 0.7400 mL | |
| 80 mM | 0.0222 mL | 0.1110 mL | 0.2220 mL | 0.5550 mL | |
| 100 mM | 0.0178 mL | 0.0888 mL | 0.1776 mL | 0.4440 mL |
LY3295668 erbumine Related Classifications
HY-114258A Related Classifications
Powered by Bioz