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

M2698 (Synonyms: MSC2363318A)

Cat. No.: HY-100501
Handling Instructions

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.

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

M2698 Chemical Structure

M2698 Chemical Structure

CAS No. : 1379545-95-5

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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].

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].

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.
Molecular Weight

449.86

Formula

C₂₁H₁₉ClF₃N₅O

CAS No.

1379545-95-5

SMILES

O=C(C1=CC=CC2=C(N[[email protected]@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

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

M2698MSC2363318AM 2698M-2698Ribosomal S6 Kinase (RSK)AktS6KPKBProtein kinase BorallypGSK3βpS6blood-brainbarrieranti-cancerATPcompetitivebreasttumorsInhibitorinhibitorinhibit

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M2698
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