1379545-95-5
1379545-95-5 structure
- Name: M2698(MSC-2363318A)
- Chemical Name: M2698
- CAS Number: 1379545-95-5
- Molecular Formula: C21H19ClF3N5O
- Molecular Weight: 449.863
- Catalog: Signaling Pathways MAPK/ERK Pathway Ribosomal S6 Kinase (RSK)
- Create Date: 2018-04-11 15:15:14
- Modify Date: 2024-01-09 21:42:37
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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].
| Name | M2698 |
|---|---|
| Synonyms |
4-[(S)-2-azetidin-1-yl-1-(4-chloro-3-trifluoromethylphenyl)ethylamino]quinazoline-8-carboxylic acid amide
MSC-2363318A |
| 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]. |
|---|---|
| Related Catalog | |
| Target |
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. |
| References |
| Molecular Formula | C21H19ClF3N5O |
|---|---|
| Molecular Weight | 449.863 |