GLPBio

LTURM34

Catalog No.: GC19227Purity:>99.00%

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

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LTURM34
Cas No.: 1879887-96-3
5mgIn Stock
$75.00
1
10mgIn Stock
$123.00
1
50mgIn Stock
$491.00
1
100mgIn Stock
$819.00
1

Citations

1 publicationsPublications from researchers using this product

Description

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

LTURM34 shows potent inhibition of DNA-PK with excellent selectivity over the Class I PI3K isoforms. The IC50s are 5.8 and 8.5 uM 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].

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.

Protocol

Kinase experiment:

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.

Product Documents

Purity:>99.00%Appearance:A solid

Chemical Properties

CAS No.
1879887-96-3
SMILES
O=C1C2=CC=CC(C3=CC=CC4=C3SC5=C4C=CC=C5)=C2OC(N6CCOCC6)=N1
Molecular Formula
C24H18N2O3S
Molecular Weight
414.48
Solubility
DMSO : ≥ 37.5 mg/mL (90.47 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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