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Merck
CN

234501

Compound 401

A cell-permeable pyrimido-isoquinolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 280 nM) with ~19-fold selectivity over mTOR (IC50 = 5.3 µM).

Synonym(s):

Compound 401, 2-(Morpholin-1-yl)pyrimido[2,1-a]isoquinolin-4-one

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About This Item

Empirical Formula (Hill Notation):
C16H15N3O2
CAS Number:
168425-64-7
Molecular Weight:
281.31
UNSPSC Code:
12352200

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InChI key

BVRDQVRQVGRNHG-UHFFFAOYSA-N

InChI

1S/C16H15N3O2/c20-15-11-14(18-7-9-21-10-8-18)17-16-13-4-2-1-3-12(13)5-6-19(15)16/h1-6,11H,7-10H2

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

beige

solubility

DMSO: 5 mg/mL

shipped in

ambient

Quality Level

100

General description

A cell-permeable pyrimido-isoquinolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 280 nM) with ~19-fold selectivity over mTOR (IC50 = 5.3 µM). Exhibits much reduced or no activity against 43 other commonly studied kinases, including PI 3-K, ATM, and ATR. Shown to induce apoptosis and inhibit mTOR-dependent growth in TSC1-/- murine embryo fibroblasts.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Ballou, L.M., et al. 2007. J. Biol. Chem.282, 24463.
Griffin, R.J., et al. 2005. J. Med. Chem.48, 569.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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