LTURM 34

Modify Date: 2024-01-13 18:26:41

LTURM 34 Structure
LTURM 34 structure
Common Name LTURM 34
CAS Number 1879887-96-3 Molecular Weight 414.476
Density 1.4±0.1 g/cm3 Boiling Point 657.8±65.0 °C at 760 mmHg
Molecular Formula C24H18N2O3S Melting Point N/A
MSDS N/A Flash Point 351.6±34.3 °C

 Use of LTURM 34


LTURM34 is a specific DNA-PK inhibitor with an IC50 of 0.034 μM.

 Names

Name LTURM34
Synonym More Synonyms

 LTURM 34 Biological Activity

Description LTURM34 is a specific DNA-PK inhibitor with an IC50 of 0.034 μM.
Related Catalog
Target

DNA-PK:34 nM (IC50)

PI3Kβ:5.8 μM (IC50)

PI4Kδ:8.5 μM (IC50)

In Vitro LTURM34 shows potent inhibition of DNA-PK with excellent selectivity over the Class I PI3K isoforms. The IC50s are 5.8 and 8.5 μM for PI3K β and δ, respectively. LTURM34 shows potent and broad ranging antiproliferative activity. LTURM34 is more consistently active against the selected cell lines (11 of 16), but at best shows 54% inhibition against the HOP-92 non-small cell lung cancer line[1].
Kinase Assay LTURM34 is dissolved at 10 mM in DMSO and stored at -20°C until use. PI3K enzyme activity is determined in 50 μL of 20 mM HEPES pH 7.5, 5 mM MgCl2 with 180 μM PI and 10 μM ATP. After a 60 min incubation at room temperature the reaction is stopped by the addition of 50 μl of Kinase-Glo followed by a further 15 min incubation. Luminescence is then read using a luostar plate reader. LTURM34 is diluted in 20% (v/v) DMSO at the ndicated concentrations in order to generate a concentration versus inhibition of enzyme activity curve which is then analysed using GraphPad Prism version 5.00 for Windows, in order to calculate the IC50[1].
References

[1]. Morrison R, et al. Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines. Eur J Med Chem. 2016 Mar 3;110:326-39.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 657.8±65.0 °C at 760 mmHg
Molecular Formula C24H18N2O3S
Molecular Weight 414.476
Flash Point 351.6±34.3 °C
Exact Mass 414.103821
LogP 3.97
Vapour Pressure 0.0±2.0 mmHg at 25°C
Index of Refraction 1.742
Storage condition -20℃

 Synonyms

8-(Dibenzo[b,d]thiophen-4-yl)-2-(4-morpholinyl)-4H-1,3-benzoxazin-4-one
4H-1,3-Benzoxazin-4-one, 8-(dibenzo[b,d]thien-4-yl)-2-(4-morpholinyl)-