Compound 401 | Dual DNA-PK/mTOR inhibitor

CAS:
 168425-64-7
Catalog Number:
 10-3055
Compound 401 chemical structure

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Compound 401 (168425-64-7) is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR), IC50s = 0.28 and 5.3 µM respectively, with selectivity over PI3K, ATM, and ATR.1 Treatment of cells with 401 (10 µM) blocked the phosphorylation of sites modified by mTOR-Raptor and mTOR-Rictor complexes (ribosomal protein S6 kinase 1 Thr(389) and Akt Ser(473), respectively) with no direct inhibition of Akt Thr(308) phosphorylation, which is dependent on PI3K.2

References/Citations:

  1. Griffen et al. (2005), Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro; J. Med. Chem. 48 569
  2. Ballou et al. (2007), Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one; J. Biol. Chem. 282 24463
168425-64-7, Compound 401, Compound 401 supplier, Dual DNA-PK and mTOR inhibitor
CAS:
168425-64-7
Catalog Number:
10-3055
Activity:
Dual DNA-PK/mTOR inhibitor
Chemical Names:
2-(4-Morpholinyl)-4H-pyrimido[2,1-a]isoquinolin-4-one
Molecular Weight:
281.32
Molecular Formula:

C16H15N3O2

Solubility:
Soluble in DMSO (6 mg/ml with warming)
Physical Properties:
Off-white solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ room temperature. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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Compound 401 (168425-64-7) is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR), IC50s = 0.28 and 5.3 µM respectively, with selectivity over PI3K, ATM, and ATR.1 Treatment of cells with 401 (10 µM) blocked the phosphorylation of sites modified by mTOR-Raptor and mTOR-Rictor complexes (ribosomal protein S6 kinase 1 Thr(389) and Akt Ser(473), respectively) with no direct inhibition of Akt Thr(308) phosphorylation, which is dependent on PI3K.2

References/Citations:

  1. Griffen et al. (2005), Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro; J. Med. Chem. 48 569
  2. Ballou et al. (2007), Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one; J. Biol. Chem. 282 24463

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