| Identification | Back Directory | [Name]
M2698 | [CAS]
1379545-95-5 | [Synonyms]
M2698
M2698 (MSC-2363318A)
M2698; M-2698; M 2698; MSC-2363318A; MSC 2363318A; MSC2363318A
(S)-4-(2-(azetidin-1-yl)-1-(4-chloro-3-(trifluoromethyl)phenyl)ethylamino)quinazoline-8-carboxamide
8-Quinazolinecarboxamide, 4-[[(1S)-2-(1-azetidinyl)-1-[4-chloro-3-(trifluoromethyl)phenyl]ethyl]amino]-
4-[(S)-2-azetidin-1-yl-1-(4-chloro-3-trifluoromethylphenyl)ethylamino]quinazoline-8-carboxylic acid amide | [Molecular Formula]
C21H19ClF3N5O | [MDL Number]
MFCD31744446 | [MOL File]
1379545-95-5.mol | [Molecular Weight]
449.86 |
| Chemical Properties | Back Directory | [solubility ]
DMSO: soluble | [form ]
A solid | [color ]
White to off-white | [InChIKey]
HXAUJHZZPCBFPN-QGZVFWFLSA-N | [SMILES]
N1=C2C(C=CC=C2C(N)=O)=C(N[C@@H](C2=CC=C(Cl)C(C(F)(F)F)=C2)CN2CCC2)N=C1 |
| Hazard Information | Back Directory | [Uses]
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]. | [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].
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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].
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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].
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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.
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| [IC 50]
p70S6K: 1 nM (IC50); Akt1: 1 nM (IC50); Akt3: 1 nM (IC50) | [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. PMID:27186432 |
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