M2698 free base · Synonyms: M-2698

M2698 is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor.

For research use only. Not for human or veterinary use.

Target Ribosomal S6 Kinase (RSK) Akt

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

M2698 structure

CAS No.: 1379545-95-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 500.00	BP-02489-50mg	In stock	Get quote
100 mg	USD 800.00	BP-02489-100mg	In stock	Get quote
250 mg	USD 1,600.00	BP-02489-250mg	In stock	Get quote
500 mg	USD 2,560.00	BP-02489-500mg	In stock	Get quote
1 g	USD 4,100.00	BP-02489-1g	In stock	Get quote
2 g	Inquire	BP-02489-2g	In stock	Inquire
3 g	USD 7,860.00	BP-02489-3g	In stock	Get quote

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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 .

Biological activity

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. ? 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. ? M2698 inhibits indirectly pGSK3β (IC50=17 nM) and pS6 (IC50=15 nM). 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. ? 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. ? 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. ? 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.

Identifiers

SMILES: NC(=O)C1=C2N=CN=C(N[C@H](CN3CCC3)C3=CC(=C(Cl)C=C3)C(F)(F)F)C2=CC=C1
InChIKey: HXAUJHZZPCBFPN-QGZVFWFLSA-N

Specifications

MW (average): 449.8570
Formula: C₂₁H₁₉ClF₃N₅O
CAS No.: 1379545-95-5
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, protect from light, stored under nitrogen; In solvent -20°C, 1 year;

Solubility

Soluble in DMSO

Documents

References

[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.

Same target

Search Ribosomal S6 Kinase (RSK)

Same research area

Search Cancer