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Purity: ≥98%
GSK1324726A (I-BET726; GSK-1324726A), a tetrahydroquinoline analog, is a novel and potent ApoA1 up-regulator and selective BET Bromodomain inhibitor with anticancerand anti-inflammatory activity. It inhibits BRD2/3/4 with IC50s of 41 nM, 31 nM, and 22 nM, respectively. It has potent in vitro antiproliferative and anti-inflammatory effects which translate into in vivo efficacy in oncology and inflammation models.
| ln Vitro |
panel of neuroblastoma cell lines are treated with GSK1324726A (I-BET726), and reported substantial growth suppression and cytotoxicity in most cell lines irrespective of MYCN copy number or expression level. All neuroblastoma cell lines studied exhibit significant growth inhibition, with a median growth IC50 value (gIC50; inhibitor concentration resulting in 50% growth inhibition) equal to 75 nM[1].
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| ln Vivo |
I-BET726 (GSK1324726A) suppresses the growth of neuroblastoma tumors. Because of the extent of the tumor, the mice in the vehicle group in the SK-N-AS model are put to death on day 14. On day 14 of the research, 58% tumor growth inhibition (TGI) is found in the GSK1324726A (15 mg/kg) group, whereas there is no significant difference in tumor growth between the vehicle and GSK1324726A (5 mg/kg) groups (n=9; p=0.006). The GSK1324726A (15 mg/kg) group of mice receive treatment for an additional 7 days until the tumor volume equals that of the vehicle group. At that time, the study is stopped. In the CHP-212 model, tumor growth is substantially slower. At the end of the trial (Day 14), 42 days later, the tumors in the mice treated with vehicle are barely half the size of those in the SK-N-AS model. Treatment with 5 mg/kg GSK1324726A in the CHP-212 model causes TGI to equal 50% (n=8; p=0.1816), while mice in the 15 mg/kg group show a TGI of 82% at study's conclusion (n=5; p=0.0488)[1].
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| References |
[1]. Wyce A, et al. BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models. PLoS One. 2013 Aug 23;8(8):e72967.
[2]. Gosmini R, et al. The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. J Med Chem. 2014 Oct 9;57(19):8111-31 |
| Molecular Formula |
C25H23CLN2O3
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| Molecular Weight |
434.91
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| CAS # |
1300031-52-0
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| Related CAS # |
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| SMILES |
ClC1=CC=C(N[C@H]2C3=C(C=CC(C4=CC=C(C(O)=O)C=C4)=C3)N(C(C)=O)[C@@H](C)C2)C=C1
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| Chemical Name |
4-[(2S,4R)-1-Acetyl-4-[(4-chlorophenyl)amino]-2-methyl-1,2,3,4-tetrahydro-6-quinolinyl]benzoic acid
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| Synonyms |
GSK1324726A, I-BET726, I-BET-726, I-BET 726, GSK-1324726A, GSK 1324726A
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2993 mL | 11.4966 mL | 22.9933 mL | |
| 5 mM | 0.4599 mL | 2.2993 mL | 4.5987 mL | |
| 10 mM | 0.2299 mL | 1.1497 mL | 2.2993 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
I-BET726: a novel selective inhibitor of BET family proteins.PLoS One. 2013; 8(8): e72967. |
I-BET726 treatment results in potent growth inhibition and cytotoxicity in neuroblastoma cell lines.PLoS One. 2013; 8(8): e72967. |
Global transcript profiling in neuroblastoma cell lines treated with I-BET726 reveals gene expression changes in apoptotic and signaling pathways.PLoS One. 2013; 8(8): e72967. |
Suppression of BCL2 expression by I-BET726.PLoS One. 2013; 8(8): e72967. |
MYCNexpression is directly regulated by BRD4 and repressed by treatment with I-BET726.PLoS One. 2013; 8(8): e72967. |
Analysis of I-BET726 activityin vivo.PLoS One. 2013; 8(8): e72967. |
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