Referencia número: HY-100501

M2698

(Synonyms: MSC2363318A)

1 Cited Publications

Revisión del cliente

Based on 1 publication(s) in Google Scholar

M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC₅₀s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity.

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Pureza: 99.74%
No. CAS: 1379545-95-5
Fòrmula: C₂₁H₁₉ClF₃N₅O
Peso molecular:449.86

Almacenamiento:

-20°C, protect from light, stored under nitrogen

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

M2698 Chemical Structure

No. CAS: 1379545-95-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (1)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

p70S6K

1 nM (IC₅₀)

Akt1

1 nM (IC₅₀)

Akt3

1 nM (IC₅₀)

Ver todos los productos específicos de isoformas Ribosomal S6 Kinase (RSK) :

Ver todos los productos específicos de isoformas Akt :

In Vitro

M2698 (0.3 nM to 50 M; 72 hours) inhibits proliferation in a dose-dependent manner in breast tumors cell lines with IC₅₀s of 0.02-8.5 μM^[1].
? M2698 (0.3, 1 μM; 24 hours) inhibits p70S6K activity and induces feedback loop phosphorylation on Akt and suppresses Akt activity in breast cancer cell lines^[1].
? M2698 inhibits indirectly pGSK3β (IC₅₀=17 nM) and pS6 (IC₅₀=15 nM)^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

Breast tumors cell lines
Concentration:

0.3 nM to 50 M
Incubation Time:

72 hours
Result:

Inhibited proliferation in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:

HCC1419 and MDA-MB-453 cells
Concentration:

0.3, 1 µM
Incubation Time:

24 hours
Result:

Inhibited p70S6K activity and induced feedback loop phosphorylation on Akt and suppressed Akt activity in breast cancer cell lines.

In Vivo

M2698 (10-30 mg/kg/day; PO; 28 days) results in dose-dependent inhibition of tumor growth and results in tumor regression with the highest dose of 30 mg/kg^[1].
? M2698 (20 mg/kg/day; PO; 4 days) has a tumor:plasma exposure ratio of 12:1 over 24 hours and leads to increased levels of pAkt in tumor tissue^[1].
? The mean total concentration of M2698 after 16-hour infusion in rats is 1750 ng/g and 175 ng/mL in brain and plasma, respectively^[1].
? M2698 (po; 1, 5, 10, or 20 mg/kg/day; for 7 days) inhibits the phosphorylation of S6 in a dose-proportional manner over time after a single administration or daily treatments over 7 days^[1].

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

Animal Model:

Female nude mice bearing MDA-MB-468 tumors^[1]
Dosage:

10, 20 and 30 mg/kg
Administration:

PO; daily; for 28 days
Result:

Resulted in dose-dependent inhibition of tumor growth and resulted in tumor regression with the highest dose of 30 mg/kg.

Animal Model:

Female SCID Beige mice with MDA-MB-453 xenografted^[1]
Dosage:

20 mg/kg (Pharmacokinetic Analysis)
Administration:

Daily; for 4 days
Result:

Had a tumor:plasma exposure ratio of 12:1 over 24 hours.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1379545-95-5
Appearance Solid
Peso molecular 449.86
Fòrmula C₂₁H₁₉ClF₃N₅O
Color White to off-white
SMILES

O=C(C1=CC=CC2=C(N[C@@H](C3=CC=C(Cl)C(C(F)(F)F)=C3)CN4CCC4)N=CN=C12)N
Synonyms

MSC2363318A
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

-20°C, protect from light, stored under nitrogen

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

Publications (1)

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Journal Impact Factor

Nat Chem Biol

Pharmacodynamics of Akt drugs revealed by a kinase-modulated bioluminescent indicator. [Abstract]

2025 Aug;21(8):1194-1204. PMID: 39934397

Solvente y solubilidad

In Vitro:

DMSO : 125 mg/mL (277.86 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

2.2229 mL

11.1146 mL

22.2291 mL

5 mM

0.4446 mL

2.2229 mL

4.4458 mL

10 mM

0.2223 mL

1.1115 mL

2.2229 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 (protect from light, 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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: ≥ 2.08 mg/mL (4.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (282 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Machl A, et al. M2698 is a potent dual-inhibitor of p70S6K and Akt that affects tumor growth in mouse models of cancer and crosses the blood-brain barrier. Am J Cancer Res. 2016 Mar 15;6(4):806-18. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2229 mL	11.1146 mL	22.2291 mL	55.5728 mL
	5 mM	0.4446 mL	2.2229 mL	4.4458 mL	11.1146 mL
	10 mM	0.2223 mL	1.1115 mL	2.2229 mL	5.5573 mL
	15 mM	0.1482 mL	0.7410 mL	1.4819 mL	3.7049 mL
	20 mM	0.1111 mL	0.5557 mL	1.1115 mL	2.7786 mL
	25 mM	0.0889 mL	0.4446 mL	0.8892 mL	2.2229 mL
	30 mM	0.0741 mL	0.3705 mL	0.7410 mL	1.8524 mL
	40 mM	0.0556 mL	0.2779 mL	0.5557 mL	1.3893 mL
	50 mM	0.0445 mL	0.2223 mL	0.4446 mL	1.1115 mL
	60 mM	0.0370 mL	0.1852 mL	0.3705 mL	0.9262 mL
	80 mM	0.0278 mL	0.1389 mL	0.2779 mL	0.6947 mL
	100 mM	0.0222 mL	0.1111 mL	0.2223 mL	0.5557 mL

M2698

1 Cited Publications

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M2698

Immunology/Inflammation Compound Library

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Anti-Breast Cancer Compound Library

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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

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

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) M2698

Ver todos los productos específicos de isoformas Ribosomal S6 Kinase (RSK)

Ver todos los productos específicos de isoformas Akt

Actividad biológica

Chemical Information

Publications (1)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

M2698 Related Classifications

HY-100501 Related Classifications