Cat. No.: HY-151504

Engasertib

(Synonyms: ALM301)

2 Cited Publications

Customer Review

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.

For research use only. We do not sell to patients.

Purity: 99.65%
CAS No.: 1313439-71-2
Formula: C₂₅H₂₅N₃O₃
Molecular Weight:415.48

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Engasertib Chemical Structure

CAS No.: 1313439-71-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

AKT1

0.13 μM (IC₅₀)

Akt2

0.09 μM (IC₅₀)

Akt3

2.75 μM (IC₅₀)

All Akt Isoforms :

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.

Cell Proliferation Assay^[1]

Cell Line:

MCF-7, T47D, NCI-H460, HCT116 and other cancer cells
Concentration:

0.001-10 µM
Incubation Time:

72 h
Result:

Inhibited the proliferation of cancer cells, and PI3KCA-mutant MCF-7 cells was the most sensitive with an IC₅₀ of 2.25 µM.

Western Blot Analysis^[1]

Cell Line:

MCF-7
Concentration:

0.001-10 µM
Incubation Time:

1, 4, 24 and 48 h
Result:

Inhibited pAKT and pGSK3β at various concentrations and timepoints up to 48 h.

In Vivo

ALM301 (10, 30 and 100 mg/kg; p.o.; single dosage) inhibits pAKT^S473 in tumors and suppresses tumor growth^[1].
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.

Animal Model:

BALB/c mice (bearing A549 xenografts)^[1]
Dosage:

10, 30 and 100 mg/kg
Administration:

p.o.; single dosage
Result:

Increased total plasma concentrations dose-dependently that resulted in almost total abrogation of measurable pAKT^S473 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.

Animal Model:

BALB/c mice (bearing PIK3CA-mutant MCF-7 xenografts)^[1]
Dosage:

3 or 10 mg/kg
Administration:

p.o.; q.d. for 49 days
Result:

Showed significant tumour regressions of 57% and 50% at 3 and 10 mg/kg, respectively, when combined with Tamoxifen (HY-13757A) (5 mg/kg; q.d.).

Chemical Information

CAS No. 1313439-71-2
Appearance Solid
Molecular Weight 415.48
Formula C₂₅H₂₅N₃O₃
Color Off-white to light yellow
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
Synonyms

ALM301
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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

Solvent & Solubility

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4069 mL

12.0343 mL

24.0685 mL

5 mM

0.4814 mL

2.4069 mL

4.8137 mL

10 mM

0.2407 mL

1.2034 mL

2.4069 mL

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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 (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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Page N, et al. Identification and development of a subtype-selective allosteric AKT inhibitor suitable for clinical development. Sci Rep. 2022 Sep 20;12(1):15715. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
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

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Engasertib

Bioactive Compound Library Max

Bioactive Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Anti-Cardiovascular Disease Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

MCE Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Engasertib

All Akt Isoforms

Biological Activity

Chemical Information

Publications (2)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Engasertib Related Classifications

HY-151504 Related Classifications