Engasertib
Based on 2 publication(s) in Google Scholar
Engasertib is an orally active highly specific AKT inhibitor with IC50 values of 0.13 µM, 0.09 µM and 2.75 µM for AKT1, AKT2 and AKT3, respectively. Engasertib inhibits AKT phosphorylation and modulates downstream signalling in vitro. Engasertib can inhibit cancer cell proliferation and tumor growth.
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- Pureté: 99.65%
- CAS No.: 1313439-71-2
- Formule: C25H25N3O3
- Masse moléculaire:415.48
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Engasertib
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Activité biologique
Description
IC50 & Target
[1]|
AKT1 0.13 μM (IC50) |
Akt2 0.09 μM (IC50) |
Akt3 2.75 μM (IC50) |
In Vitro
Engasertib (0.001-10 µM; 72 h) inhibits the proliferation of cancer cells, and PI3KCA-mutant MCF-7 cells is the most sensitive; increases sub-G0 population in a dose-dependent manner[1].
Engasertib (1 µM; 1 h) inhibits AKT phosphorylation in MCF-7 and sustains up to 48 h, with an EC50 value of 0.47 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7, T47D, NCI-H460, HCT116 and other cancer cells
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Concentration:0.001-10 µM
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Incubation Time:72 h
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Result:Inhibited the proliferation of cancer cells, and PI3KCA-mutant MCF-7 cells was the most sensitive with an IC50 of 2.25 µM.
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Cell Line:MCF-7
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Concentration:0.001-10 µM
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Incubation Time:1, 4, 24 and 48 h
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Result:Inhibited pAKT and pGSK3β at various concentrations and timepoints up to 48 h.
In Vivo
ALM301 (3 or 10 mg/kg; p.o.; q.d. for 49 days) shows better tumor inhibition ability when combined with Tamoxifen (HY-13757A)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (bearing A549 xenografts)[1]
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Dosage:10, 30 and 100 mg/kg
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Administration:p.o.; single dosage
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Result:Increased total plasma concentrations dose-dependently that resulted in almost total abrogation of measurable pAKTS473 in tumors at all timepoints over 24 h.
Exhibited the tumour growth inhibition (TGI) of 23, 31 and 41% at 10, 30 and 100 mg/kg, respectively.
Chemical Information
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CAS No. 1313439-71-2
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Appearance Solid
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Masse moléculaire 415.48
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Formule C25H25N3O3
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Color Off-white to light yellow
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SMILES
O=C1N(CC)C2=CC(C3=CC=CC=C3)=C(C4=CC=C([C@@]5(N)C[C@H](O)C5)C=C4)N=C2OC1
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Synonyms
ALM301
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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J Dig Dis
Hepatic interleukin 32 attenuates liver injury through repression of necroptosis in cholestasis. [Abstract]2023 Apr;24(4):293-304. PMID: 37261903 -
bioRxiv
A kinome inhibitor screen implicates adhesion and growth factor signaling in cellular recovery after caspase activation. [Abstract]2026 Jan 7:2026.01.06.697929. PMID: 41542583
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (120.34 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. 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. 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 (6.02 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
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
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Fiche technique (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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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. 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 |
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| DMSO | 1 mM | 2.4069 mL | 12.0343 mL | 24.0685 mL | 60.1714 mL |
| 5 mM | 0.4814 mL | 2.4069 mL | 4.8137 mL | 12.0343 mL | |
| 10 mM | 0.2407 mL | 1.2034 mL | 2.4069 mL | 6.0171 mL | |
| 15 mM | 0.1605 mL | 0.8023 mL | 1.6046 mL | 4.0114 mL | |
| 20 mM | 0.1203 mL | 0.6017 mL | 1.2034 mL | 3.0086 mL | |
| 25 mM | 0.0963 mL | 0.4814 mL | 0.9627 mL | 2.4069 mL | |
| 30 mM | 0.0802 mL | 0.4011 mL | 0.8023 mL | 2.0057 mL | |
| 40 mM | 0.0602 mL | 0.3009 mL | 0.6017 mL | 1.5043 mL | |
| 50 mM | 0.0481 mL | 0.2407 mL | 0.4814 mL | 1.2034 mL | |
| 60 mM | 0.0401 mL | 0.2006 mL | 0.4011 mL | 1.0029 mL | |
| 80 mM | 0.0301 mL | 0.1504 mL | 0.3009 mL | 0.7521 mL | |
| 100 mM | 0.0241 mL | 0.1203 mL | 0.2407 mL | 0.6017 mL |
Engasertib Related Classifications
HY-151504 Related Classifications
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