2. MAPK/ERK Pathway PI3K/Akt/mTOR
  3. Ribosomal S6 Kinase (RSK) Akt
  4. M2698

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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M2698 Chemical Structure

M2698 Chemical Structure

CAS No. : 1379545-95-5

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Based on 1 publication(s) in Google Scholar

M2698 Related Antibodies

Top Publications Citing Use of Products

View All Ribosomal S6 Kinase (RSK) Isoform Specific Products:

View All Isoforms
p70S6K RSK1 RSK2 RSK3 RSK4

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target[1]

p70S6K

1 nM (IC50)

Akt1

1 nM (IC50)

Akt3

1 nM (IC50)

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.

M2698 Related Antibodies

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.
Clinical Trial
Molecular Weight

449.86

Formula

C21H19ClF3N5O
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2229 mL 11.1146 mL 22.2291 mL
5 mM 0.4446 mL 2.2229 mL 4.4458 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 (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.

  • Molarity Calculator

  • Dilution Calculator

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: ≥ 2.08 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.

    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% 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

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 (protect from light, 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.
Purity & Documentation

Purity: 99.87%

SDS (393 KB)

COA (254 KB) HNMR (285 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

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 (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.

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
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M2698 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:

M26981379545-95-5MSC2363318AM 2698M-2698Ribosomal S6 Kinase (RSK)AktS6KPKBProtein kinase BorallypGSK3βpS6blood-brainbarrieranti-cancerATPcompetitivebreasttumorsInhibitorinhibitorinhibit

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