Compound 401

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Cat.No. 3271 - Compound 401 | C16H15N3O2 | CAS No. 168425-64-7
Description: Selective DNA-PK and mTOR inhibitor
Chemical Name: 2-(4-Morpholinyl)-4H-pyrimido[2,1-a]isoquinolin-4-one
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Reversible and selective inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR) (IC50 values are 0.28 and 5.3 μM respectively). Displays little affinity for other commonly studied kinases including PI 3-K, ATM and ATR (IC50 values are all > 100 μM). Induces apoptosis in vitro.

Technical Data

M. Wt 281.31
Formula C16H15N3O2
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 168425-64-7
PubChem ID 10039361
InChI Key BVRDQVRQVGRNHG-UHFFFAOYSA-N
Smiles O=C3N2C=CC1=CC=CC=C1C2=NC(N4CCOCC4)=C3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 2.81 10
ethanol 1.41 5

Preparing Stock Solutions

The following data is based on the product molecular weight 281.31. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 35.55 mL 177.74 mL 355.48 mL
0.5 mM 7.11 mL 35.55 mL 71.1 mL
1 mM 3.55 mL 17.77 mL 35.55 mL
5 mM 0.71 mL 3.55 mL 7.11 mL

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References

References are publications that support the biological activity of the product.

Griffen et al (2005) Selective benzopyranone and pyrimido[2,1-α]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 PMID: 15658870

Ballo et al (2007) Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)oyrimido[2,1-α]isoquinolin-4-one. J.Biol.Chem. 282 24463 PMID: 17562705


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