LTURM34 |
Catalog No.GC19227
One-Click Copy Product Info
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LTURM34 is a specific DNA-PK inhibitor with an IC50 of 0.034 uM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1879887-96-3
Sample solution is provided at 25 µL, 10mM.
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.
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. | |
| Cas No. | 1879887-96-3 | SDF | |
| Canonical SMILES | O=C1C2=CC=CC(C3=CC=CC4=C3SC5=C4C=CC=C5)=C2OC(N6CCOCC6)=N1 | ||
| Formula | C24H18N2O3S | M.Wt | 414.48 |
| Solubility | DMSO : ≥ 37.5 mg/mL (90.47 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4127 mL | 12.0633 mL | 24.1266 mL |
| 5 mM | 482.5 μL | 2.4127 mL | 4.8253 mL |
| 10 mM | 241.3 μL | 1.2063 mL | 2.4127 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)